AU2011224316B2 - Heterocyclic inhibitors of histamine receptors for the treatment of disease - Google Patents

Heterocyclic inhibitors of histamine receptors for the treatment of disease Download PDF

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Publication number
AU2011224316B2
AU2011224316B2 AU2011224316A AU2011224316A AU2011224316B2 AU 2011224316 B2 AU2011224316 B2 AU 2011224316B2 AU 2011224316 A AU2011224316 A AU 2011224316A AU 2011224316 A AU2011224316 A AU 2011224316A AU 2011224316 B2 AU2011224316 B2 AU 2011224316B2
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chosen
compound
mmol
salt
thiophen
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AU2011224316A
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AU2011224316A1 (en
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Allen Borchardt
Robert Davis
Stewart A. Noble
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Kalypsys Inc
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Kalypsys Inc
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    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2011224316A 2010-03-10 2011-03-10 Heterocyclic inhibitors of histamine receptors for the treatment of disease Ceased AU2011224316B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31261510P 2010-03-10 2010-03-10
US61/312,615 2010-03-10
PCT/US2011/027817 WO2011112766A2 (en) 2010-03-10 2011-03-10 Heterocyclic inhibitors of histamine receptors for the treatment of disease

Publications (2)

Publication Number Publication Date
AU2011224316A1 AU2011224316A1 (en) 2012-09-13
AU2011224316B2 true AU2011224316B2 (en) 2016-09-15

Family

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AU2011224316A Ceased AU2011224316B2 (en) 2010-03-10 2011-03-10 Heterocyclic inhibitors of histamine receptors for the treatment of disease

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US (1) US8569300B2 (enExample)
EP (1) EP2545058B1 (enExample)
JP (1) JP5888654B2 (enExample)
KR (1) KR20130016253A (enExample)
CN (1) CN102869666B (enExample)
AR (1) AR080496A1 (enExample)
AU (1) AU2011224316B2 (enExample)
BR (1) BR112012022211A2 (enExample)
CA (1) CA2791417A1 (enExample)
ES (1) ES2607125T3 (enExample)
IL (1) IL221829A (enExample)
MX (1) MX2012010404A (enExample)
NZ (1) NZ602041A (enExample)
PH (1) PH12012501783A1 (enExample)
RU (1) RU2012137180A (enExample)
TW (1) TW201200518A (enExample)
UY (1) UY33271A (enExample)
WO (1) WO2011112766A2 (enExample)

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US8859550B2 (en) * 2011-09-12 2014-10-14 Kalypsys, Inc. Heterocyclic inhibitors of histamine receptors for the treatment of disease
US9266891B2 (en) 2012-11-16 2016-02-23 Boehringer Ingelheim International Gmbh Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors
MD20150103A2 (ro) 2013-05-02 2016-02-29 Pfizer Inc. Derivaţi ai imidazo-triazinei ca inhibitori ai PDE10
EP3290407B1 (en) 2013-10-18 2020-01-01 Celgene Quanticel Research, Inc Bromodomain inhibitors
WO2015123424A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
LT3105218T (lt) 2014-02-13 2019-12-10 Incyte Corp Ciklopropilaminai kaip lsd1 inhibitoriai
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
WO2016007722A1 (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
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BR112020009757A2 (pt) * 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
US11498930B2 (en) 2018-02-13 2022-11-15 Blueray Therapeutics (Shanghai) Co., Ltd Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
CN115448923B (zh) * 2018-02-13 2024-03-22 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CN110655520A (zh) * 2018-06-29 2020-01-07 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
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AR080496A1 (es) 2012-04-11
PH12012501783A1 (en) 2015-06-26
WO2011112766A3 (en) 2012-01-19
WO2011112766A2 (en) 2011-09-15
KR20130016253A (ko) 2013-02-14
CN102869666A (zh) 2013-01-09
EP2545058A4 (en) 2013-07-24
US20110237565A1 (en) 2011-09-29
UY33271A (es) 2011-10-31
IL221829A (en) 2014-11-30
ES2607125T3 (es) 2017-03-29
BR112012022211A2 (pt) 2017-07-18
RU2012137180A (ru) 2014-04-20
NZ602041A (en) 2014-08-29
US8569300B2 (en) 2013-10-29
AU2011224316A1 (en) 2012-09-13
JP5888654B2 (ja) 2016-03-22
TW201200518A (en) 2012-01-01
CA2791417A1 (en) 2011-09-15
CN102869666B (zh) 2015-09-09
EP2545058B1 (en) 2016-08-24
EP2545058A2 (en) 2013-01-16
MX2012010404A (es) 2013-05-20
JP2013522222A (ja) 2013-06-13

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