CA2539853C - Isoquinolinone potassium channel inhibitors - Google Patents

Isoquinolinone potassium channel inhibitors Download PDF

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Publication number
CA2539853C
CA2539853C CA2539853A CA2539853A CA2539853C CA 2539853 C CA2539853 C CA 2539853C CA 2539853 A CA2539853 A CA 2539853A CA 2539853 A CA2539853 A CA 2539853A CA 2539853 C CA2539853 C CA 2539853C
Authority
CA
Canada
Prior art keywords
methyl
methoxy
phenylisoquinolin
compound
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2539853A
Other languages
English (en)
French (fr)
Other versions
CA2539853A1 (en
Inventor
Christopher J. Dinsmore
Jeffrey M. Bergman
Charles J. Mcintyre
David A. Claremon
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.)
Individual
Original Assignee
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of CA2539853A1 publication Critical patent/CA2539853A1/en
Application granted granted Critical
Publication of CA2539853C publication Critical patent/CA2539853C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
    • A61K31/535Heterocyclic 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
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632Organic additives
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Manufacturing & Machinery (AREA)
  • Ceramic Engineering (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Materials Engineering (AREA)
  • Structural Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2539853A 2003-09-23 2004-09-17 Isoquinolinone potassium channel inhibitors Expired - Fee Related CA2539853C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50521403P 2003-09-23 2003-09-23
US60/505,214 2003-09-23
PCT/US2004/030470 WO2005046578A2 (en) 2003-09-23 2004-09-17 Isoquinolinone potassium channel inhibitors

Publications (2)

Publication Number Publication Date
CA2539853A1 CA2539853A1 (en) 2005-05-26
CA2539853C true CA2539853C (en) 2011-04-19

Family

ID=34590091

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2539853A Expired - Fee Related CA2539853C (en) 2003-09-23 2004-09-17 Isoquinolinone potassium channel inhibitors

Country Status (7)

Country Link
US (1) US7709476B2 (enExample)
EP (1) EP1667978B1 (enExample)
JP (1) JP4719151B2 (enExample)
CN (1) CN1856474A (enExample)
AU (1) AU2004289186B2 (enExample)
CA (1) CA2539853C (enExample)
WO (1) WO2005046578A2 (enExample)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763614B2 (en) * 2003-09-23 2010-07-27 Merck Sharp & Dohme Corp. Isoquinoline potassium channel inhibitors
CN1856473A (zh) * 2003-09-23 2006-11-01 默克公司 异喹啉酮钾通道抑制剂
ATE476419T1 (de) * 2003-09-23 2010-08-15 Merck Sharp & Dohme Isochinolinon-kaliumkanalinhibitoren
JP4718467B2 (ja) * 2003-09-23 2011-07-06 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリノンカリウムチャネル阻害剤
US7723290B2 (en) 2004-10-22 2010-05-25 Bioincept, Llc Compositions and methods for modulating the immune system
DE102005028862A1 (de) * 2005-06-22 2007-01-11 Sanofi-Aventis Deutschland Gmbh Substituierte Heterocyclen, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
GB0525164D0 (en) 2005-12-09 2006-01-18 Xention Discovery Ltd Compounds
BRPI0716715B1 (pt) * 2006-08-23 2021-07-06 Xenon Pharmaceuticals, Inc Derivados de 4-(n-azacicloalquil) anilidas como moduladores de canal de potássio, seus usos, produto, composição, comprimido e cápsula
GB0815782D0 (en) 2008-08-29 2008-10-08 Xention Ltd Novel potassium channel blockers
GB0815781D0 (en) 2008-08-29 2008-10-08 Xention Ltd Novel potassium channel blockers
GB0815784D0 (en) 2008-08-29 2008-10-08 Xention Ltd Novel potassium channel blockers
US8883852B2 (en) 2008-10-22 2014-11-11 University of Pittburgh—Of the Commonwealth System of Higher Education Radioprotective agents
EP2845856A1 (en) 2009-06-29 2015-03-11 Incyte Corporation Pyrimidinones as PI3K inhibitors
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
JP6166858B2 (ja) * 2011-03-02 2017-07-19 バイオインセプト、エルエルシー 細胞内損傷の治療のための組成物および方法
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
UA121539C2 (uk) 2011-09-02 2020-06-25 Інсайт Холдинґс Корпорейшн Гетероцикліламіни як інгібітори рі3к
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
UA122332C2 (uk) 2015-02-27 2020-10-26 Інсайт Корпорейшн Солі інгібітора pi3k і способи їх отримання
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
EP3341739A4 (en) 2015-08-28 2019-07-10 BioIncept LLC MUTATED PEPTIDES AND METHOD FOR TREATING SUBJECTS THEREWITH
EP3341006A4 (en) 2015-08-28 2019-03-13 BioIncept LLC COMPOSITIONS AND METHODS FOR TREATING NERVE DAMAGE
MX2020012826A (es) 2018-06-01 2021-03-09 Incyte Corp Regimen de dosificacion para el tratamiento de trastornos relacionados con fosfatidilinositol 3-cinasas (pi3k).

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2888289A (en) * 1988-01-27 1989-07-27 May & Baker Limited Isoquinolinones
JP3724818B2 (ja) * 1992-09-04 2005-12-07 武田薬品工業株式会社 縮合複素環化合物、その製造法および剤
ATE161530T1 (de) * 1992-09-04 1998-01-15 Takeda Chemical Industries Ltd Kondensierte heterozyklische verbindungen, deren herstellung und verwendung
JPH0776573A (ja) * 1993-07-14 1995-03-20 Takeda Chem Ind Ltd ヘテロ環化合物、その製造法および剤
EP0634402A1 (en) * 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
US5387685A (en) 1993-07-16 1995-02-07 American Cyanamid Co MDR reversal agents
AU2001269516B2 (en) * 2000-07-13 2006-09-14 Takeda Pharmaceutical Company Limited Lipid-rich plaque regressing agents
JP4854909B2 (ja) * 2000-09-20 2012-01-18 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリノン系カリウムチャンネル阻害剤
JP4213390B2 (ja) * 2001-02-02 2009-01-21 武田薬品工業株式会社 縮合複素環化合物
PE20021002A1 (es) * 2001-02-02 2002-12-06 Takeda Chemical Industries Ltd Compuestos heterociclicos condensados
WO2003068750A1 (en) * 2002-02-13 2003-08-21 Takeda Chemical Industries, Ltd. Jnk inhibitor
JP4718467B2 (ja) * 2003-09-23 2011-07-06 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリノンカリウムチャネル阻害剤
CN1856473A (zh) * 2003-09-23 2006-11-01 默克公司 异喹啉酮钾通道抑制剂
US7763614B2 (en) * 2003-09-23 2010-07-27 Merck Sharp & Dohme Corp. Isoquinoline potassium channel inhibitors
ATE476419T1 (de) * 2003-09-23 2010-08-15 Merck Sharp & Dohme Isochinolinon-kaliumkanalinhibitoren

Also Published As

Publication number Publication date
AU2004289186A1 (en) 2005-05-26
CA2539853A1 (en) 2005-05-26
AU2004289186B2 (en) 2010-12-16
EP1667978A4 (en) 2007-08-29
US20080227778A1 (en) 2008-09-18
JP4719151B2 (ja) 2011-07-06
CN1856474A (zh) 2006-11-01
US7709476B2 (en) 2010-05-04
EP1667978A2 (en) 2006-06-14
EP1667978B1 (en) 2013-09-04
WO2005046578A2 (en) 2005-05-26
JP2007506740A (ja) 2007-03-22
WO2005046578A3 (en) 2005-09-15

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Effective date: 20150917