EA200900285A1 - Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов - Google Patents

Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов

Info

Publication number
EA200900285A1
EA200900285A1 EA200900285A EA200900285A EA200900285A1 EA 200900285 A1 EA200900285 A1 EA 200900285A1 EA 200900285 A EA200900285 A EA 200900285A EA 200900285 A EA200900285 A EA 200900285A EA 200900285 A1 EA200900285 A1 EA 200900285A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
activating enzymes
compounds
compounds used
heteroaryl compounds
Prior art date
Application number
EA200900285A
Other languages
English (en)
Other versions
EA024793B1 (ru
Inventor
Кристофер Ф. Клейборн
Стефен Критчли
Стивен П. Лэнгстон
Эдвард Дж. Олава
Стефан Пелюсо
Габриэл С. Везерхед
Степан Вискочил
Айраш Визиерс
Хиротаке Мицутани
Кортни Каллис
Original Assignee
Миллениум Фармасьютикалз, Инк.
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 Миллениум Фармасьютикалз, Инк. filed Critical Миллениум Фармасьютикалз, Инк.
Publication of EA200900285A1 publication Critical patent/EA200900285A1/ru
Publication of EA024793B1 publication Critical patent/EA024793B1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61P17/06—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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Это изобретение относится к соединениям, которые ингибируют активирующие ферменты Е1, к фармацевтическим композициям, содержащим эти соединения, и к способам применения соединений. Эти соединения используются для лечения нарушений, в частности нарушений разрастания клеток, в том числе раковых, воспалительных и нейродегенеративных нарушений; и воспаления, связанного с инфекцией и кахексией.
EA200900285A 2006-08-08 2007-08-06 Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов EA024793B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83615806P 2006-08-08 2006-08-08
PCT/US2007/017463 WO2008019124A1 (en) 2006-08-08 2007-08-06 Heteroaryl compounds useful as inhibitors of e1 activating enzymes

Publications (2)

Publication Number Publication Date
EA200900285A1 true EA200900285A1 (ru) 2009-08-28
EA024793B1 EA024793B1 (ru) 2016-10-31

Family

ID=38669274

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201501088A EA201501088A1 (ru) 2006-08-08 2007-08-06 Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов
EA200900285A EA024793B1 (ru) 2006-08-08 2007-08-06 Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201501088A EA201501088A1 (ru) 2006-08-08 2007-08-06 Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов

Country Status (30)

Country Link
EP (1) EP2049491B1 (ru)
JP (4) JP5274460B2 (ru)
KR (3) KR101538103B1 (ru)
CN (2) CN103923021B (ru)
AR (1) AR062270A1 (ru)
AT (1) ATE485276T1 (ru)
AU (1) AU2007281993B2 (ru)
BR (1) BRPI0715176A8 (ru)
CA (1) CA2659894C (ru)
CO (1) CO6150159A2 (ru)
CY (1) CY1111121T1 (ru)
DE (1) DE602007009998D1 (ru)
DK (1) DK2049491T3 (ru)
EA (2) EA201501088A1 (ru)
ES (1) ES2354925T3 (ru)
HK (1) HK1130803A1 (ru)
HR (1) HRP20110017T1 (ru)
IL (4) IL196845A (ru)
ME (1) ME02789B (ru)
MX (1) MX2009001309A (ru)
MY (1) MY157177A (ru)
NO (1) NO20090434L (ru)
NZ (1) NZ574513A (ru)
PL (1) PL2049491T3 (ru)
PT (1) PT2049491E (ru)
RS (1) RS51549B (ru)
SI (1) SI2049491T1 (ru)
TW (2) TWI472516B (ru)
WO (1) WO2008019124A1 (ru)
ZA (1) ZA200900670B (ru)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2562245C2 (ru) * 2009-05-14 2015-09-10 Милленниум Фармасьютикалз, Инк. ГИДРОХЛОРИД (1S,2S,4R)-4-{ 4-[(1S)-2,3-ДИГИДРО-1Н-ИНДЕН-1-ИЛАМИНО]-7Н-ПИРРОЛО [2,3-d]ПИРИМИДИН-7-ИЛ} -2-ГИДРОКСИЦИКЛОПЕНТИЛ)МЕТИЛ СУЛЬФАМАТА
RU2809821C2 (ru) * 2019-06-13 2023-12-19 Шанхай Инститьют Оф Материа Медика, Чайниз Академи Оф Сайенсиз Соединения на основе триазолопиримидина и их соли, композиции на их основе и пути их применения

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8933225B2 (en) * 2007-08-02 2015-01-13 Millennium Pharmaceuticals, Inc. Process for the synthesis of E1 activating enzyme inhibitors
AU2013204618B2 (en) * 2007-08-02 2015-11-05 Takeda Pharmaceutical Company Limited Process for the synthesis of E1 activating enzyme inhibitors
CA2987743A1 (en) 2009-03-13 2010-09-16 Katholieke Universiteit Leuven, K.U.Leuven R&D Purine derivatives and their use as immunosuppressive agents
KR20130001272A (ko) * 2010-03-17 2013-01-03 에프. 호프만-라 로슈 아게 이미다조피리딘 및 푸린 화합물, 조성물 및 사용 방법
GB201012889D0 (en) 2010-08-02 2010-09-15 Univ Leuven Kath Antiviral activity of novel bicyclic heterocycles
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
GB201015411D0 (en) 2010-09-15 2010-10-27 Univ Leuven Kath Anti-cancer activity of novel bicyclic heterocycles
AU2012298813B2 (en) 2011-08-24 2016-07-28 Millennium Pharmaceuticals, Inc. Inhibitors of Nedd8-activating enzyme
WO2013052814A2 (en) * 2011-10-07 2013-04-11 Millennium Pharmaceuticals, Inc. E1 enzyme mutants and uses thereof
JP6238900B2 (ja) 2011-10-28 2017-11-29 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｎａｅ阻害物質に対する応答のバイオマーカー
MX357835B (es) 2011-11-03 2018-07-26 Millennium Pharm Inc Administración de inhibidor de enzimas que activa nedd8 y agente de hipometilación.
UA117095C2 (uk) 2011-12-22 2018-06-25 Аліос Біофарма, Інк. Нуклеозидна сполука або її фармацевтично прийнятна сіль
KR20140123104A (ko) 2012-02-17 2014-10-21 밀레니엄 파머슈티컬스 인코퍼레이티드 유비퀴틴 활성화 효소의 피라졸로피리미디닐 억제제
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
EP2674432A1 (en) 2012-06-14 2013-12-18 LEK Pharmaceuticals d.d. New synthetic route for the preparation of ß aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]pyrazin-7-yl compounds
CN104822844B (zh) 2012-10-01 2019-05-07 米伦纽姆医药公司 预测对抑制剂的反应的生物标记物和方法以及其用途
CN104918939B (zh) * 2012-11-16 2018-08-28 默沙东公司 人磷脂酰肌醇3-激酶δ的嘌呤抑制剂
EP2764866A1 (en) * 2013-02-07 2014-08-13 IP Gesellschaft für Management mbH Inhibitors of nedd8-activating enzyme
EP2996773B1 (en) 2013-05-14 2020-09-16 Millennium Pharmaceuticals, Inc. Administration of nedd8-activating enzyme inhibitor and chemotherapeutic agents
WO2015002994A2 (en) * 2013-07-02 2015-01-08 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of sumo activating enzyme
US9334273B1 (en) 2014-03-05 2016-05-10 University Of Georgia Research Foundation, Inc. Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA)
DK3164130T3 (da) * 2014-07-01 2019-10-28 Millennium Pharm Inc Heteroaryle forbindelser anvendelige som inhibatorer af sumo-aktiverende enzym
CN105061220A (zh) * 2015-08-26 2015-11-18 吴玲 一种制备r-3-甲基-1-氨基茚满的方法
CN105111091A (zh) * 2015-08-26 2015-12-02 吴玲 制备s-3-甲基-1-氨基茚满的方法
CN105085279A (zh) * 2015-08-26 2015-11-25 吴玲 制备r-5-氯-1-氨基茚满
CN105130824A (zh) * 2015-08-31 2015-12-09 吴玲 一种制备s-5-溴-1-氨基茚满的方法
US20200377958A1 (en) 2017-12-01 2020-12-03 Millennium Pharmaceuticals, Inc. Biomarkers and methods for treatment with nae inhibitors
KR20210106506A (ko) 2018-12-21 2021-08-30 셀진 코포레이션 Ripk2의 티에노피리딘 억제제
US11198699B2 (en) 2019-04-02 2021-12-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
CN110229067A (zh) * 2019-06-05 2019-09-13 南京焕然生物科技有限公司 一种2-氨基茚制备方法
US11540867B2 (en) 2019-08-13 2023-01-03 Pioneer Surgical Technology, Inc. Driver for a bone screw
CN110563655A (zh) * 2019-09-24 2019-12-13 上海毕得医药科技有限公司 一种5-（2-溴乙基）嘧啶的制备方法
KR20220124176A (ko) 2019-12-06 2022-09-13 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 조절제로서의 치환된 테트라하이드로푸란
CR20220484A (es) * 2020-02-28 2022-12-15 Remix Therapeutics Inc Amidas heterocíclicas y su uso para modular el empalme
AU2022284886A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels
WO2023021498A1 (en) * 2021-08-16 2023-02-23 Moya Bio Ltd. Fused azole and furan based nucleoside analogs and uses thereof
CN115124534B (zh) * 2021-11-23 2023-09-15 中山大学 非核苷酸类prmt5小分子抑制剂、制备方法及用途
WO2024067676A1 (zh) * 2022-09-30 2024-04-04 微境生物医药科技(上海)有限公司 作为sumo活化酶抑制剂的化合物
WO2024099438A1 (zh) * 2022-11-11 2024-05-16 微境生物医药科技(上海)有限公司 作为sumo活化酶抑制剂的化合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0714957B2 (ja) * 1987-03-09 1995-02-22 理化学研究所 ２′−デオキシ−５−フルオロウリジン誘導体及び制癌剤
AU6500696A (en) * 1995-07-28 1997-02-26 Cubist Pharmaceuticals, Inc. Aminoacyl adenylate mimics as novel antimicrobial and antiparasitic agents
AU2003291024A1 (en) * 2002-11-13 2004-06-03 Rigel Pharmaceuticals, Inc. Rhodanine derivatives and pharmaceutical compositions containing them
WO2005037845A1 (en) * 2003-10-17 2005-04-28 Rigel Pharmaceuticals, Inc. Benzothiazole and thiazole[5,5-b] pyridine compositions and their use as ubiquitin ligase inhibitors
JP4643156B2 (ja) * 2004-03-02 2011-03-02 独立行政法人科学技術振興機構 Ｎ−アシルスルホンアミド結合を有する新規ホスミドシン類縁体
EP1758873A1 (en) * 2004-06-22 2007-03-07 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
CA2596424C (en) * 2005-02-04 2016-03-29 Millennium Pharmaceuticals, Inc. Inhibitors of e1 activating enzymes
CN101379061B (zh) * 2006-02-02 2016-06-15 千禧药品公司 E1活化酶抑制剂

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2562245C2 (ru) * 2009-05-14 2015-09-10 Милленниум Фармасьютикалз, Инк. ГИДРОХЛОРИД (1S,2S,4R)-4-{ 4-[(1S)-2,3-ДИГИДРО-1Н-ИНДЕН-1-ИЛАМИНО]-7Н-ПИРРОЛО [2,3-d]ПИРИМИДИН-7-ИЛ} -2-ГИДРОКСИЦИКЛОПЕНТИЛ)МЕТИЛ СУЛЬФАМАТА
RU2809821C2 (ru) * 2019-06-13 2023-12-19 Шанхай Инститьют Оф Материа Медика, Чайниз Академи Оф Сайенсиз Соединения на основе триазолопиримидина и их соли, композиции на их основе и пути их применения

Also Published As

Publication number Publication date
JP2013100368A (ja) 2013-05-23
TWI472516B (zh) 2015-02-11
CY1111121T1 (el) 2015-06-11
IL242112A0 (en) 2015-11-30
DK2049491T3 (da) 2011-02-14
PL2049491T3 (pl) 2011-04-29
IL242113A0 (en) 2015-11-30
EP2049491A1 (en) 2009-04-22
JP5906297B2 (ja) 2016-04-20
CN101516850A (zh) 2009-08-26
AU2007281993B2 (en) 2013-08-29
ME02789B (me) 2011-06-30
JP5274460B2 (ja) 2013-08-28
NZ574513A (en) 2012-02-24
BRPI0715176A2 (pt) 2013-06-11
EA024793B1 (ru) 2016-10-31
JP2015013904A (ja) 2015-01-22
ES2354925T3 (es) 2011-03-21
IL196845A0 (en) 2009-11-18
MY157177A (en) 2016-05-13
EA201501088A1 (ru) 2017-01-30
KR101538103B1 (ko) 2015-07-22
SI2049491T1 (sl) 2011-05-31
CN103923021A (zh) 2014-07-16
HK1130803A1 (en) 2010-01-08
CN103923021B (zh) 2018-03-30
ATE485276T1 (de) 2010-11-15
KR20150036358A (ko) 2015-04-07
HRP20110017T1 (hr) 2011-02-28
IL254784A0 (en) 2017-12-31
WO2008019124A1 (en) 2008-02-14
DE602007009998D1 (de) 2010-12-02
PT2049491E (pt) 2011-01-26
ZA200900670B (en) 2010-04-28
MX2009001309A (es) 2009-02-13
KR101555258B1 (ko) 2015-09-24
IL242112A (en) 2017-10-31
AR062270A1 (es) 2008-10-29
WO2008019124A8 (en) 2014-01-30
TWI515181B (zh) 2016-01-01
CA2659894C (en) 2018-03-27
CN101516850B (zh) 2014-05-07
CO6150159A2 (es) 2010-04-20
KR20140066753A (ko) 2014-06-02
BRPI0715176A8 (pt) 2018-04-10
EP2049491B1 (en) 2010-10-20
KR20090038931A (ko) 2009-04-21
JP2010500353A (ja) 2010-01-07
JP2016106157A (ja) 2016-06-16
TW201439065A (zh) 2014-10-16
AU2007281993A1 (en) 2008-02-14
CA2659894A1 (en) 2008-02-14
TW200815369A (en) 2008-04-01
NO20090434L (no) 2009-02-16
IL196845A (en) 2015-11-30
RS51549B (en) 2011-06-30

Similar Documents

Publication Publication Date Title
EA200900285A1 (ru) Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов
EA200801784A1 (ru) Ингибиторы е1 активирующих ферментов
MY149957A (en) Heterocyclic inhibitors of mek and methods of use thereof
EA200901212A1 (ru) 3-имидазолилиндолы, предназначенные для лечения пролиферативных заболеваний
MX2009006706A (es) Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
EA201200951A1 (ru) Определенные триазолопиридины и триазолопиразины, их композиции и способы их применения
WO2012088266A3 (en) Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
EA201000797A1 (ru) Аминотриазолы в качестве ингибиторов pi3k
EA201170531A1 (ru) Соединения на основе пиридина и пиримидина в качестве ингибиторов сигнального пути wnt для лечения рака
CL2008001633A1 (es) Compuestos derivados de pirrolidin-3-carboxamida; composición farmacéutica; y uso comominhibidores de erk para el tratamiento del cancer.
EA201200323A1 (ru) Соединения и композиции, как ингибиторы протеинкиназы
BRPI0917017B8 (pt) inibidores de pirrol de s-nitrosoglutationa redutase como agentes terapêuticos
EA201170521A1 (ru) Новые соединения
EP2321264A4 (en) DEACETYLASEINHIBITORS AND APPLICATIONS THEREOF
EA200800664A1 (ru) Производные пирролопиримидина в качестве ингибиторов syk
MA32393B1 (fr) Composés et compositions servant d'inhibiteurs de kinases
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201170832A1 (ru) Пуриновые соединения
WO2008086462A3 (en) AMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS INHIBITORS OF β-CANTENIN/TCF-4 PATHWAY AND CANCER TREATMENT AGENTS
EA201171435A1 (ru) Твердые фармацевтические композиции и способы их получения
EA201691032A1 (ru) Производные изохромена в качестве ингибиторов фосфоинозитид-3-киназ
BRPI0914305B8 (pt) compostos de piridazina carboxamida substituída como compostos inibidores da quinase, uso dos compostos e uso de uma composição compreendendo os compostos
ATE540036T1 (de) Heterocyclische derivate als ionenkanalmodulatoren
EA201201676A1 (ru) Гетероарильные соединения и композиции в качестве ингибиторов протеинкиназы
MX2013002398A (es) Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.

Legal Events

Date Code Title Description
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

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): RU