CN104203914B - 作为lsd1抑制剂的(杂)芳基环丙胺化合物 - Google Patents

作为lsd1抑制剂的(杂)芳基环丙胺化合物 Download PDF

Info

Publication number
CN104203914B
CN104203914B CN201280063757.4A CN201280063757A CN104203914B CN 104203914 B CN104203914 B CN 104203914B CN 201280063757 A CN201280063757 A CN 201280063757A CN 104203914 B CN104203914 B CN 104203914B
Authority
CN
China
Prior art keywords
compound
ring
formula
group
phenylcyclopropyl
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.)
Active
Application number
CN201280063757.4A
Other languages
English (en)
Chinese (zh)
Other versions
CN104203914A (zh
Inventor
阿尔贝托·奥尔特加·穆诺兹
马修·科林·索尔·法伊夫
佩德蒙特 马克·马丁内尔
马丁内斯 玛丽亚·德·洛斯·安赫莱斯·艾斯蒂亚尔特
比达尔 努里亚·巴利斯
吉多·库尔茨
帕洛米诺 拉里亚 胡利奥·塞萨尔·卡斯特罗
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.)
Oryzon Genomics SA
Original Assignee
Oryzon Genomics SA
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 Oryzon Genomics SA filed Critical Oryzon Genomics SA
Priority to CN201710469023.0A priority Critical patent/CN107266345B/zh
Publication of CN104203914A publication Critical patent/CN104203914A/zh
Application granted granted Critical
Publication of CN104203914B publication Critical patent/CN104203914B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic 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 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
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/96Spiro-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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 nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/56Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96Sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20Spiro-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/12Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
    • C07D309/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D335/00Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Biotechnology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Quinoline Compounds (AREA)
  • Pyrane Compounds (AREA)
CN201280063757.4A 2011-10-20 2012-10-22 作为lsd1抑制剂的(杂)芳基环丙胺化合物 Active CN104203914B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710469023.0A CN107266345B (zh) 2011-10-20 2012-10-22 作为lsd1抑制剂的(杂)芳基环丙胺化合物

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
EP11382325 2011-10-20
EP11382325.6 2011-10-20
EP11382331 2011-10-27
EP11382331.4 2011-10-27
US201161558365P 2011-11-10 2011-11-10
US201161558367P 2011-11-10 2011-11-10
US61/558,367 2011-11-10
US61/558,365 2011-11-10
PCT/EP2012/070898 WO2013057320A1 (en) 2011-10-20 2012-10-22 (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201710469023.0A Division CN107266345B (zh) 2011-10-20 2012-10-22 作为lsd1抑制剂的(杂)芳基环丙胺化合物

Publications (2)

Publication Number Publication Date
CN104203914A CN104203914A (zh) 2014-12-10
CN104203914B true CN104203914B (zh) 2017-07-11

Family

ID=48140381

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201280063757.4A Active CN104203914B (zh) 2011-10-20 2012-10-22 作为lsd1抑制剂的(杂)芳基环丙胺化合物
CN201710469023.0A Expired - Fee Related CN107266345B (zh) 2011-10-20 2012-10-22 作为lsd1抑制剂的(杂)芳基环丙胺化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201710469023.0A Expired - Fee Related CN107266345B (zh) 2011-10-20 2012-10-22 作为lsd1抑制剂的(杂)芳基环丙胺化合物

Country Status (12)

Country Link
US (3) US9487512B2 (enExample)
EP (2) EP2768805B1 (enExample)
JP (2) JP6215212B2 (enExample)
KR (1) KR102139537B1 (enExample)
CN (2) CN104203914B (enExample)
AU (2) AU2012324803B9 (enExample)
BR (1) BR112014009306B1 (enExample)
CA (1) CA2852355C (enExample)
IL (1) IL232102A (enExample)
MX (1) MX356344B (enExample)
RU (1) RU2681211C2 (enExample)
WO (1) WO2013057320A1 (enExample)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
BR112012006572A2 (pt) 2009-09-25 2016-04-26 Oryzon Genomics Sa inibidores de demetilase-1 de lisina específicos e seu uso
EP2486002B1 (en) 2009-10-09 2019-03-27 Oryzon Genomics, S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
US9616058B2 (en) 2010-02-24 2017-04-11 Oryzon Genomics, S.A. Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use
WO2011106106A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
JP5868948B2 (ja) 2010-04-19 2016-02-24 オリゾン・ジェノミックス・ソシエダッド・アノニマOryzon Genomics S.A. リジン特異的脱メチル化酵素1阻害薬およびその使用
ES2674747T3 (es) 2010-07-29 2018-07-03 Oryzon Genomics, S.A. Inhibidores de demetilasa LSD1 basados en arilciclopropilamina y sus usos médicos
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) * 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
EP3981395A1 (en) * 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
PH12013501871A1 (en) 2011-03-25 2019-06-03 Glaxosmithkline Ip No 2 Ltd Cyclopropylamines as lsd1 inhibitors
EP2768805B1 (en) 2011-10-20 2020-03-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
RU2668952C2 (ru) 2011-10-20 2018-10-05 Оризон Дженомикс, С.А. (гетеро)арилциклопропиламины в качестве ингибиторов lsd1
US10323012B2 (en) * 2012-06-05 2019-06-18 Hong Kong Baptist University Miliusanes as antiviral agents
WO2014058071A1 (ja) * 2012-10-12 2014-04-17 武田薬品工業株式会社 シクロプロパンアミン化合物およびその用途
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
WO2014194280A2 (en) * 2013-05-30 2014-12-04 The Board of Regents of the Nevada System of Higher Education on behalf of the University of Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells
WO2015021128A1 (en) 2013-08-06 2015-02-12 Imago Biosciences Inc. Kdm1a inhibitors for the treatment of disease
TWI720451B (zh) 2014-02-13 2021-03-01 美商英塞特控股公司 作為lsd1抑制劑之環丙胺
WO2015123437A1 (en) * 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9670210B2 (en) 2014-02-13 2017-06-06 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9487511B2 (en) 2014-04-11 2016-11-08 Takeda Pharmaceutical Company Limited Cyclopropanamine compound and use thereof
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
ES2686326T3 (es) 2014-07-15 2018-10-17 Grünenthal GmbH Derivados de azaspiro(4,5)decano sustituidos
TW201607923A (zh) 2014-07-15 2016-03-01 歌林達有限公司 被取代之氮螺環(4.5)癸烷衍生物
CN107438593B (zh) * 2015-01-30 2020-10-30 基因泰克公司 治疗化合物及其用途
HRP20250119T1 (hr) 2015-02-12 2025-03-28 Imago Biosciences Inc. Kdm1a inhibitor i njegova primjena u terapiji
MX373154B (es) 2015-04-03 2020-04-22 Incyte Holdings Corp Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1).
CN106045862B (zh) * 2015-04-10 2019-04-23 上海迪诺医药科技有限公司 环丙胺类螺(杂)环化合物、其药物组合物及应用
US10526287B2 (en) 2015-04-23 2020-01-07 Constellation Pharmaceuticals, Inc. LSD1 inhibitors and uses thereof
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
CA2987876A1 (en) 2015-06-12 2016-12-15 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
US10059668B2 (en) 2015-11-05 2018-08-28 Mirati Therapeutics, Inc. LSD1 inhibitors
SG11201805645QA (en) 2015-12-29 2018-07-30 Mirati Therapeutics Inc Lsd1 inhibitors
CA3009709A1 (en) 2015-12-30 2017-07-06 Novartis Ag Immune effector cell therapies with enhanced efficacy
CN110267945A (zh) * 2016-03-01 2019-09-20 诺华股份有限公司 氰基取代的吲哚化合物及其作为lsd1抑制剂的用途
CA3253937A1 (en) 2016-03-15 2025-03-04 Oryzon Genomics, S.A. Combinations of Lysine-Specific Demethylase 1 Inhibitors for the Treatment of Hematological Maligna
EA201892075A1 (ru) 2016-03-15 2019-04-30 Оризон Дженомикс, С.А. Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей
CN107200706A (zh) * 2016-03-16 2017-09-26 中国科学院上海药物研究所 一类氟取代的环丙胺类化合物及其制备方法、药物组合物和用途
US11034991B2 (en) 2016-03-16 2021-06-15 Oryzon Genomics S.A. Methods to determine KDM1A target engagement and chemoprobes useful therefor
UA125559C2 (uk) 2016-04-22 2022-04-20 Інсайт Корпорейшн Композиції інгібітора lsd1
ES2732669T3 (es) 2016-06-10 2019-11-25 Oryzon Genomics Sa Tratamiento de la esclerosis múltiple
WO2018020366A1 (en) * 2016-07-26 2018-02-01 Glaxosmithkline Intellectual Property (No.2) Limited Crystalline (r)-mandelate salt of (1r,2s)-2-phenylcyclopropylamine
CN111194306B (zh) 2016-08-16 2023-05-16 伊美格生物科学公司 用于制备kdm1a抑制剂的方法和过程
EP3532459B1 (en) 2016-10-26 2023-08-02 Constellation Pharmaceuticals, Inc. Lsd1 inhibitors and medical uses thereof
WO2018081342A1 (en) * 2016-10-26 2018-05-03 Constellation Pharmaceuticals, Inc. Lsd1 inhibitors and uses thereof
WO2018083189A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
US12435128B2 (en) 2017-05-31 2025-10-07 Taiho Pharmaceutical Co., Ltd. Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1
JP2020152641A (ja) * 2017-07-07 2020-09-24 国立研究開発法人理化学研究所 リジン特異的脱メチル化酵素1阻害活性を有する新規化合物、その製造方法及びその用途
LT3661510T (lt) 2017-08-03 2025-01-27 Oryzon Genomics, S.A. Elgesio pakitimų gydymo būdai
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
CN109745309B (zh) * 2017-11-03 2022-01-28 香港浸会大学 作为抗病毒剂的密瘤杀
US11578059B2 (en) 2018-05-11 2023-02-14 Imago Biosciences. Inc. KDM1A inhibitors for the treatment of disease
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
CN112672994B (zh) * 2018-09-13 2022-09-13 南昌弘益药业有限公司 作为lsd1抑制剂的杂螺环类化合物及其应用
EP3851440A4 (en) * 2018-09-13 2022-06-08 Helioeast Pharmaceutical Co., Ltd. Cyclopropylamine compound as lsd1 inhibitor and use thereof
WO2020138398A1 (ja) * 2018-12-28 2020-07-02 国立研究開発法人理化学研究所 リジン特異的脱メチル化酵素1を阻害する新規化合物、その製造方法及びその用途
CN120837494A (zh) 2019-03-20 2025-10-28 奥莱松基因组股份有限公司 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法
SG11202109159VA (en) 2019-03-20 2021-10-28 Oryzon Genomics Sa Methods of treating borderline personality disorder
CN112110936B (zh) * 2019-06-20 2021-12-07 沈阳药科大学 四氢喹啉类衍生物及其制备方法和应用
WO2021004610A1 (en) 2019-07-05 2021-01-14 Oryzon Genomics, S.A. Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors
CN114502561B (zh) * 2019-09-29 2023-12-26 南昌弘益药业有限公司 Lsd1抑制剂
BR112022008020A2 (pt) 2019-11-13 2022-07-12 Taiho Pharmaceutical Co Ltd Métodos de tratamento de doenças e distúrbios relacionados a lsd1 com inibidores de lsd1
EP3964204A1 (en) 2020-09-08 2022-03-09 Université d'Aix-Marseille Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues
CN112451671B (zh) * 2020-12-02 2021-11-02 武汉大学 KDM1A在抑制RNA病毒刺激下干扰素IFNβ表达中的应用
WO2022171044A1 (zh) * 2021-02-09 2022-08-18 南昌弘益药业有限公司 一种氧氮杂螺环化合物、其盐型及其晶型
CN113750095B (zh) * 2021-03-10 2023-07-04 中国医学科学院医药生物技术研究所 含有环丙基骨架的化合物在制备治疗和/或预防冠状病毒感染药物中的应用
CN113797199B (zh) * 2021-03-31 2023-05-26 中国医学科学院医药生物技术研究所 含有环丙基骨架的甲基转移酶抑制剂在治疗黄病毒属病毒感染药物中的应用
KR20230167102A (ko) 2021-04-08 2023-12-07 오리존 지노믹스 에스.에이. 골수성 암 치료를 위한 lsd1 억제제의 조합물
CN113200967B (zh) * 2021-05-07 2022-05-24 中国人民解放军陆军军医大学 吲哚苯醌类化合物、其制备方法及其应用
JP2023147179A (ja) * 2022-03-29 2023-10-12 大日精化工業株式会社 抗ウイルス剤、抗ウイルス性樹脂組成物、及び抗ウイルス性物品
JP2025516648A (ja) 2022-05-09 2025-05-30 オリゾン・ゲノミクス・ソシエダッド・アノニマ Lsd1阻害薬を用いるnf1変異腫瘍の治療法
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100324147A1 (en) * 2009-06-02 2010-12-23 Mccafferty Dewey G Arylcyclopropylamines and methods of use
WO2011035941A1 (en) * 2009-09-25 2011-03-31 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
WO2011106105A2 (en) * 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011131697A1 (en) * 2010-04-19 2011-10-27 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
WO2012013728A1 (en) * 2010-07-29 2012-02-02 Oryzon Genomics S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use

Family Cites Families (143)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR901228A (fr) 1943-01-16 1945-07-20 Deutsche Edelstahlwerke Ag Système d'aimant à entrefer annulaire
GB913385A (en) 1960-09-01 1962-12-19 Ici Ltd Esters of diboronic acids
US3106578A (en) 1960-09-16 1963-10-08 Smith Kline French Lab Nu-phenethyl-2-phenylcyclopropylamine derivatives
US3365458A (en) 1964-06-23 1968-01-23 Aldrich Chem Co Inc N-aryl-n'-cyclopropyl-ethylene diamine derivatives
US3532749A (en) 1965-05-11 1970-10-06 Aldrich Chem Co Inc N'-propargyl-n**2-cyclopropyl-ethylenediamines and the salts thereof
US3532712A (en) 1967-09-29 1970-10-06 Aldrich Chem Co Inc N'-cyclopropyl ethylenediamine derivatives
US3471522A (en) 1967-09-29 1969-10-07 Aldrich Chem Co Inc N-cyclopropyl-n'-furfuryl-n'-methyl ethylene diamines
US3654306A (en) 1970-01-26 1972-04-04 Robins Co Inc A H 5-azaspiro(2.4)heptane-4 6-diones
US3758684A (en) 1971-09-07 1973-09-11 Burroughs Wellcome Co Treating dna virus infections with amino purine derivatives
US4530901A (en) 1980-01-08 1985-07-23 Biogen N.V. Recombinant DNA molecules and their use in producing human interferon-like polypeptides
JPS59357B2 (ja) 1981-02-20 1984-01-06 富士通株式会社 洗滌用グロ−ブボツクス天井の防滴構造
US4617389A (en) 1981-05-15 1986-10-14 University Patents, Inc. Mitomycin analogs
NZ199617A (en) * 1981-05-15 1985-08-30 University Patents Inc Azirino(2',3',:3,4)pyrrolo(1,2-a)indole-4,7-dione derivatives and pharmaceutical compositions
US4409243A (en) 1981-11-09 1983-10-11 Julian Lieb Treatment of auto-immune and inflammatory diseases
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
GB9311282D0 (en) 1993-06-01 1993-07-21 Rhone Poulenc Rorer Ltd New compositions of matter
DE69535461T2 (de) 1994-10-21 2008-09-25 NPS Pharmaceuticals, Inc., Salt Lake City Kalzium-rezeptor aktive verbindungen
US5652258A (en) 1995-05-30 1997-07-29 Gliatech, Inc. 2-(4-imidazoyl) cyclopropyl derivatives
US20040132820A1 (en) 1996-02-15 2004-07-08 Jean Gosselin Agents with leukotriene B4-like antiviral (DNA) and anti-neoplastic activities
GB9615730D0 (en) 1996-07-26 1996-09-04 Medical Res Council Anti-viral agent 1
US5961987A (en) 1996-10-31 1999-10-05 University Of Iowa Research Foundation Ocular protein stimulants
DE19647615A1 (de) 1996-11-18 1998-05-20 Bayer Ag Verfahren zur Herstellung von Cyclopropylaminen
SE9702772D0 (sv) 1997-07-22 1997-07-22 Astra Pharma Prod Novel compounds
TW530058B (en) 1997-07-22 2003-05-01 Astra Pharma Prod Triazolo [4,5-d]pyrimidine compounos and their use and process for preparation
AU1631699A (en) 1997-12-18 1999-07-05 E.I. Du Pont De Nemours And Company Cyclohexylamine arthropodicides and fungicides
US6809120B1 (en) 1998-01-13 2004-10-26 University Of Saskatchewan Technologies Inc. Composition containing propargylamine for enhancing cancer therapy
WO1999054440A1 (en) 1998-04-21 1999-10-28 Micromet Gesellschaft Für Biomedizinische Forschung Mbh CD19xCD3 SPECIFIC POLYPEPTIDES AND USES THEREOF
SE9802206D0 (sv) 1998-06-22 1998-06-22 Astra Pharma Inc Novel compounds
TWI229674B (en) 1998-12-04 2005-03-21 Astra Pharma Prod Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses
IL152726A0 (en) 2000-05-26 2003-06-24 Schering Corp Adenosine a2a receptor antagonists
JP2001354563A (ja) 2000-06-09 2001-12-25 Sankyo Co Ltd 置換ベンジルアミン類を含有する医薬
JP2001354363A (ja) 2000-06-13 2001-12-25 Kanebo Ltd 結束帯が取り付けられた電気機器
US8519005B2 (en) 2000-07-27 2013-08-27 Thomas N. Thomas Compositions and methods to prevent toxicity of antiinflammatory agents and enhance their efficacy
EP1193268A1 (en) 2000-09-27 2002-04-03 Applied Research Systems ARS Holding N.V. Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases
EP1373203A1 (en) 2001-03-29 2004-01-02 Bristol-Myers Squibb Company Cyclopropylindole derivatives as selective serotonin reuptake inhibitors
DE10123163A1 (de) 2001-05-09 2003-01-16 Gruenenthal Gmbh Substituierte Cyclohexan-1,4-diaminderivate
US20030008844A1 (en) 2001-05-17 2003-01-09 Keryx Biopharmaceuticals, Inc. Use of sulodexide for the treatment of inflammatory bowel disease
EP1499598A1 (en) 2002-04-18 2005-01-26 Ucb, S.A. Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
WO2003093297A2 (en) 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
US7312214B2 (en) 2002-05-10 2007-12-25 Bristol-Myers Squibb Company 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
US6951961B2 (en) 2002-05-17 2005-10-04 Marina Nikolaevna Protopopova Methods of use and compositions for the diagnosis and treatment of infectious disease
US7456222B2 (en) 2002-05-17 2008-11-25 Sequella, Inc. Anti tubercular drug: compositions and methods
US20040033986A1 (en) 2002-05-17 2004-02-19 Protopopova Marina Nikolaevna Anti tubercular drug: compositions and methods
ES2361011T3 (es) 2002-05-20 2011-06-13 Bristol-Myers Squibb Company Inhibidores del virus de la hepatitis c.
US7611704B2 (en) 2002-07-15 2009-11-03 Board Of Regents, The University Of Texas System Compositions and methods for treating viral infections using antibodies and immunoconjugates to aminophospholipids
SE0202539D0 (sv) 2002-08-27 2002-08-27 Astrazeneca Ab Compounds
US6878510B2 (en) 2002-09-10 2005-04-12 Fuji Photo Film Co., Ltd. Method of processing silver halide photosensitive material
JP2004126566A (ja) * 2002-09-10 2004-04-22 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料の処理方法
DE60318891T2 (de) 2002-12-13 2009-01-22 Smithkline Beecham Corp. Cyclopropylverbindungen als ccr5 antagonisten
SG2012000667A (en) 2003-01-08 2015-03-30 Univ Washington Antibacterial agents
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
EP1592668A1 (en) * 2003-02-12 2005-11-09 Ciba SC Holding AG Crystalline forms of pitavastatin calcium
GB0303439D0 (en) 2003-02-14 2003-03-19 Pfizer Ltd Antiparasitic terpene alkaloids
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
EP1631548B1 (en) 2003-04-24 2009-10-28 Merck & Co., Inc. Inhibitors of akt activity
CA2529036A1 (en) 2003-07-03 2005-02-03 Eli Lilly And Company Indane derivates as muscarinic receptor agonists
CN102060806A (zh) 2003-09-11 2011-05-18 iTherX药品公司 细胞因子抑制剂
EP1663193B1 (en) 2003-09-12 2012-04-04 Merck Serono SA Sulfonamide derivatives for the treatment of diabetes
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
EP1677799A4 (en) 2003-10-21 2008-09-10 Merck & Co Inc TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF FOR THE TREATMENT OF NEUROPATHIC PAIN
US7026339B2 (en) 2003-11-07 2006-04-11 Fan Yang Inhibitors of HCV NS5B polymerase
AU2004299461A1 (en) 2003-12-15 2005-06-30 Almirall Ag 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists
WO2005058808A1 (en) 2003-12-15 2005-06-30 Japan Tobacco Inc. N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof
CN1901971A (zh) 2003-12-15 2007-01-24 日本烟草产业株式会社 环丙烷化合物及其药物应用
US7399825B2 (en) 2003-12-24 2008-07-15 Lipps Binie V Synthetic peptide, inhibitor to DNA viruses
CA2564356A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
US20090275099A1 (en) 2004-04-27 2009-11-05 Regents Of The University Of Michigan Methods and compositions for treating diseases and conditions associated with mitochondrial function
DE102004057594A1 (de) 2004-11-29 2006-06-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Substitueirte Pteridine zur Behandlung von entzündlichen Erkrankungen
AU2005322312B2 (en) 2004-12-16 2011-05-26 President And Fellows Of Harvard College Histone demethylation mediated by the nuclear amine oxidase homolog LSD1
DK1704859T3 (da) 2005-02-18 2010-11-22 Universitaetsklinikum Freiburg Kontrol af androgen receptor-afhængig genenkspression ved inhibering af amin-oxidase-aktiviteten af lysin-specifik demetylase (LSD1)
US20060275366A1 (en) 2005-06-02 2006-12-07 Schering Corporation Controlled-release formulation
US7273882B2 (en) 2005-06-21 2007-09-25 Bristol-Myers Squibb Company Aminoacetamide acyl guanidines as β-secretase inhibitors
EP1741708A1 (en) 2005-06-28 2007-01-10 Sanofi-Aventis Deutschland GmbH Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
NZ565059A (en) 2005-07-25 2011-08-26 Intermune Inc Novel macrocyclic inhibitors of hepatitus C virus replication
WO2007021839A2 (en) 2005-08-10 2007-02-22 Johns Hopkins University Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors
US20090203750A1 (en) 2005-08-24 2009-08-13 Alan Kozikowski 5-HT2C Receptor Agonists as Anorectic Agents
GB0517740D0 (en) 2005-08-31 2005-10-12 Novartis Ag Organic compounds
WO2007035873A1 (en) 2005-09-21 2007-03-29 Pharmacopeia, Inc. Purinone derivatives for treating neurodegenerative diseases
TW200745067A (en) 2006-03-14 2007-12-16 Astrazeneca Ab Novel compounds
DE602007003343D1 (de) 2006-05-18 2009-12-31 Syngenta Ltd Neue mikrobiozide
US8198301B2 (en) 2006-07-05 2012-06-12 Hesheng Zhang Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors
CA2658484A1 (en) 2006-07-20 2008-01-24 Vical Incorporated Compositions and methods for vaccinating against hsv-2
WO2008033466A2 (en) 2006-09-14 2008-03-20 Combinatorx (Singapore) Pre. Ltd. Compositions and methods for treatment of viral diseases
US20110092601A1 (en) 2007-04-13 2011-04-21 The Johns Hopkins University Lysine-specific demethylase inhibitors
US7906513B2 (en) 2007-04-26 2011-03-15 Enanta Pharmaceuticals, Inc. Hydrazide-containing hepatitis C serine protease inhibitors
BRPI0813244B8 (pt) 2007-06-27 2021-05-25 Astrazeneca Ab compostos derivados de pirazinona, composições compreendendo ditos compostos, uso dos compostos no tratamento de doenças de pulmão e composto intermediário
MX2010001650A (es) 2007-08-10 2010-08-02 Glaxosmithkline Llc Entidades quimicas biciclicas que contienen nitrogeno para el tratamiento de infecciones virales.
WO2009039134A1 (en) 2007-09-17 2009-03-26 Abbott Laboratories Anti-infective pyrimidines and uses thereof
US20100016262A1 (en) 2007-10-18 2010-01-21 Yale University Compositions and methods for reducing hepatotoxicity associated with drug administration and treating non-alcoholic fatty liver disease, non-alcoholic steatohepatitis and associated cirrhosis
EP2215065B1 (en) 2007-10-19 2012-07-11 Boehringer Ingelheim International GmbH Ccr10 antagonists
CA2710417A1 (en) 2007-12-26 2009-07-02 Shionogi & Co., Ltd. Glycosylated glycopeptide antibiotic derivatives
WO2009109991A2 (en) 2008-01-23 2009-09-11 Sun Pharma Advanced Research Company Ltd., Novel hydrazide containing tyrosine kinase inhibitors
MX2010008202A (es) 2008-01-28 2010-12-06 Janssen Pharmaceutica Nv Derivados de tio-2-aminoquinolina 6-sustituida utiles como inhibidores de beta-secretasa (bace).
AU2009225647C1 (en) 2008-03-19 2015-11-19 Aurimmed Pharma, Inc. Novel compounds advantageous in the treatment of central nervous system diseases and disorders
EP2502907B1 (de) 2008-03-27 2018-08-29 Grünenthal GmbH Substituierte 4-Aminocyclohexan-Derivate
WO2010014921A2 (en) 2008-08-01 2010-02-04 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services A3 adenosine receptor antagonists and partial agonists
CA2723205C (en) 2008-04-16 2017-03-14 Portola Pharmaceuticals, Inc. 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors
EP2303889A1 (en) 2008-06-18 2011-04-06 F. Hoffmann-La Roche AG Halo-substituted pyrimidodiazepines as plkl inhibitors
EP2317992A2 (en) 2008-07-24 2011-05-11 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Preventing or treating viral infection using an inhibitor of the lsd1 protein, a mao inhibitor or an inhibitor of lsd1 and a mao inhibitor
US8130552B2 (en) 2008-09-11 2012-03-06 Sandisk Technologies Inc. Multi-pass programming for memory with reduced data storage requirement
US8048887B2 (en) 2008-09-11 2011-11-01 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
WO2010043721A1 (en) 2008-10-17 2010-04-22 Oryzon Genomics, S.A. Oxidase inhibitors and their use
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
US8299100B2 (en) 2009-01-23 2012-10-30 Northwestern University Potent and selective neuronal nitric oxide synthase inhibitors with improved membrane permeability
CA2753382C (en) 2009-02-27 2014-12-23 Enanta Pharmaceuticals, Inc. Hepatitis c virus inhibitors
PT2429995E (pt) 2009-05-15 2014-04-30 Novartis Ag Arilpiridinas como inibidores de aldosterona sintase
EP2258865A1 (en) 2009-06-05 2010-12-08 Universitätsklinikum Freiburg Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer
WO2010143582A1 (ja) 2009-06-11 2010-12-16 公立大学法人名古屋市立大学 フェニルシクロプロピルアミン誘導体及びlsd1阻害剤
US9708255B2 (en) 2009-08-18 2017-07-18 Robert A. Casero (bis)urea and (bis)thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders
WO2011031934A1 (en) 2009-09-11 2011-03-17 Enanta Pharmaceuticals, Inc. Hepatitis c virus inhibitors
EP2486002B1 (en) 2009-10-09 2019-03-27 Oryzon Genomics, S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
US8716450B2 (en) 2009-10-15 2014-05-06 Abbvie Inc. Dual variable domain immunoglobulins and uses thereof
WO2011057262A2 (en) 2009-11-09 2011-05-12 Evolva Inc. Treatment of infections with tp receptor antagonists
WO2011106106A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
WO2011113005A2 (en) 2010-03-12 2011-09-15 The Johns Hopkins University Compositions and methods for combinations of oligoamines with 2-difluoromethylornithine (dfmo)
EP2560939A2 (en) 2010-04-20 2013-02-27 Actavis Group Ptc Ehf Novel process for preparing phenylcyclopropylamine derivatives using novel intermediates
US8765820B2 (en) * 2010-04-20 2014-07-01 Universita Degli Studi Di Roma “La Sapienza” Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2
US20130165696A1 (en) 2010-06-30 2013-06-27 Actavis Group Ptc Ehf Novel processes for the preparation of phenylcyclopropylamine derivatives and use thereof for preparing ticagrelor
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
US8903602B2 (en) 2010-07-30 2014-12-02 Schrader Electronics, Ltd. Tire pressure monitoring system wheel rotation auto location
WO2012034116A2 (en) 2010-09-10 2012-03-15 The Johns Hopkins University Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders
US20130303545A1 (en) 2010-09-30 2013-11-14 Tamara Maes Cyclopropylamine derivatives useful as lsd1 inhibitors
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
US20140163041A1 (en) 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
PH12013501871A1 (en) * 2011-03-25 2019-06-03 Glaxosmithkline Ip No 2 Ltd Cyclopropylamines as lsd1 inhibitors
US20140296255A1 (en) 2011-05-19 2014-10-02 Oryzong Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
US20140329833A1 (en) 2011-05-19 2014-11-06 Oryzon Genomics, S.A Lysine demethylase inhibitors for inflammatory diseases or conditions
JP6111195B2 (ja) * 2011-08-09 2017-04-05 武田薬品工業株式会社 シクロプロパンアミン化合物
RU2668952C2 (ru) 2011-10-20 2018-10-05 Оризон Дженомикс, С.А. (гетеро)арилциклопропиламины в качестве ингибиторов lsd1
EP2768805B1 (en) * 2011-10-20 2020-03-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
CA2987876A1 (en) 2015-06-12 2016-12-15 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017060319A1 (en) 2015-10-09 2017-04-13 F. Hoffmann-La Roche Ag Gene expression biomarkers for personalized cancer care to epigenetic modifying agents
EA201892075A1 (ru) 2016-03-15 2019-04-30 Оризон Дженомикс, С.А. Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей
CA3253937A1 (en) 2016-03-15 2025-03-04 Oryzon Genomics, S.A. Combinations of Lysine-Specific Demethylase 1 Inhibitors for the Treatment of Hematological Maligna
US11034991B2 (en) 2016-03-16 2021-06-15 Oryzon Genomics S.A. Methods to determine KDM1A target engagement and chemoprobes useful therefor
EP3535414A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
WO2018083189A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100324147A1 (en) * 2009-06-02 2010-12-23 Mccafferty Dewey G Arylcyclopropylamines and methods of use
WO2011035941A1 (en) * 2009-09-25 2011-03-31 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
WO2011106105A2 (en) * 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011131697A1 (en) * 2010-04-19 2011-10-27 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
WO2012013728A1 (en) * 2010-07-29 2012-02-02 Oryzon Genomics S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors;Hanae Benelkebir,等;《Bioorganic & Medicinal Chemistry》;20110213;第19卷;第3709-3716页 *
Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B;David M. Gooden,等;《Bioorganic & Medicinal Chemistry Letters》;20080108;第18卷;第3047-3051页 *
Structurally Designed trans-2-Phenylcyclopropylamine Derivatives Potently Inhibit Histone Demethylase LSD1/KDM1;Shinya Mimasu,等;《Biochemistry》;20100622;第49卷(第30期);第6494-6503页 *

Also Published As

Publication number Publication date
AU2012324803B9 (en) 2017-08-24
CN104203914A (zh) 2014-12-10
RU2681211C2 (ru) 2019-03-05
AU2012324803B2 (en) 2017-08-03
KR102139537B1 (ko) 2020-07-31
AU2012324803A1 (en) 2014-06-05
HK1205110A1 (en) 2015-12-11
KR20140081884A (ko) 2014-07-01
WO2013057320A1 (en) 2013-04-25
BR112014009306A2 (pt) 2017-04-11
US20150025054A1 (en) 2015-01-22
MX2014004429A (es) 2015-02-10
IL232102A (en) 2017-12-31
IL232102A0 (en) 2014-05-28
US20180354902A1 (en) 2018-12-13
US20170008844A1 (en) 2017-01-12
AU2012324803A8 (en) 2014-08-14
JP2014532619A (ja) 2014-12-08
AU2017254889A1 (en) 2017-11-23
CN107266345B (zh) 2021-08-17
AU2017254889B2 (en) 2019-05-16
BR112014009306B1 (pt) 2021-07-20
JP6215212B2 (ja) 2017-10-18
JP6382403B2 (ja) 2018-08-29
CA2852355C (en) 2019-12-31
EP3736265A1 (en) 2020-11-11
US9944601B2 (en) 2018-04-17
CN107266345A (zh) 2017-10-20
MX356344B (es) 2018-05-23
CA2852355A1 (en) 2013-04-25
RU2014120210A (ru) 2015-11-27
JP2017226671A (ja) 2017-12-28
US9487512B2 (en) 2016-11-08
US10329256B2 (en) 2019-06-25
EP2768805B1 (en) 2020-03-25
EP2768805A1 (en) 2014-08-27

Similar Documents

Publication Publication Date Title
CN104203914B (zh) 作为lsd1抑制剂的(杂)芳基环丙胺化合物
US10214477B2 (en) (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors
HK1205110B (en) (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
NZ622656B2 (en) (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
HK1200457B (en) (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1205110

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1205110

Country of ref document: HK