IN2014CN03265A - - Google Patents

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Publication number
IN2014CN03265A
IN2014CN03265A IN3265CHN2014A IN2014CN03265A IN 2014CN03265 A IN2014CN03265 A IN 2014CN03265A IN 3265CHN2014 A IN3265CHN2014 A IN 3265CHN2014A IN 2014CN03265 A IN2014CN03265 A IN 2014CN03265A
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India
Prior art keywords
formula
btk kinase
compounds
disorders
vivoalkylated
Prior art date
Application number
Inventor
James John Crawford
Wendy B Young
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of IN2014CN03265A publication Critical patent/IN2014CN03265A/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • C07D405/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • 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
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    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
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    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
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    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
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  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
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  • Hematology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

in vitroin situin vivoAlkylated piperazine compounds of Formula I are provided including stereoisomers tautomers and pharmaceutically acceptable salts thereof useful for inhibiting Btk kinase and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for and diagnosis and treatment of such disorders in mammalian cells or associated pathological conditions are disclosed.
IN3265CHN2014 2011-11-03 2012-11-02 IN2014CN03265A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161555395P 2011-11-03 2011-11-03
PCT/US2012/063198 WO2013067277A1 (en) 2011-11-03 2012-11-02 Alkylated piperazine compounds as inhibitors of btk activity

Publications (1)

Publication Number Publication Date
IN2014CN03265A true IN2014CN03265A (en) 2015-07-03

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IN3265CHN2014 IN2014CN03265A (en) 2011-11-03 2012-11-02

Country Status (22)

Country Link
US (3) US8729072B2 (en)
EP (1) EP2773639B1 (en)
JP (2) JP5976828B2 (en)
KR (1) KR101716011B1 (en)
CN (1) CN104024255B (en)
AR (1) AR088642A1 (en)
AU (1) AU2012332368A1 (en)
BR (1) BR112014010439A2 (en)
CA (1) CA2853970A1 (en)
CL (1) CL2014001158A1 (en)
CO (1) CO6950475A2 (en)
CR (1) CR20140187A (en)
EA (1) EA027561B1 (en)
IL (1) IL232280A0 (en)
IN (1) IN2014CN03265A (en)
MA (1) MA35725B1 (en)
MX (1) MX2014005289A (en)
PE (1) PE20141686A1 (en)
SG (1) SG11201401993RA (en)
TW (1) TW201326171A (en)
WO (1) WO2013067277A1 (en)
ZA (1) ZA201403158B (en)

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JP2022522153A (en) 2019-02-25 2022-04-14 グアンジョウ・ルペン・ファーマシューティカル・カンパニー・リミテッド Inhibitors of BTK and its variants
CN114364798A (en) 2019-03-21 2022-04-15 欧恩科斯欧公司 Combination of Dbait molecules with kinase inhibitors for the treatment of cancer
WO2021066958A1 (en) 2019-10-05 2021-04-08 Newave Pharmaceutical Inc. Inhibitor of btk and mutants thereof
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
BR112022016432A2 (en) 2020-02-20 2022-11-16 Hutchison Medipharma Ltd HETEROARYL COMPOUNDS AND USES THEREOF
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MX2023003183A (en) 2020-09-21 2023-04-12 Hutchison Medipharma Ltd Heteroaryl heterocyclic compounds and uses thereof.
WO2022094172A2 (en) 2020-10-30 2022-05-05 Newave Pharmaceutical Inc. Inhibitors of btk
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