ES2573497T3 - Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos - Google Patents

Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos Download PDF

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Publication number
ES2573497T3
ES2573497T3 ES12704985.6T ES12704985T ES2573497T3 ES 2573497 T3 ES2573497 T3 ES 2573497T3 ES 12704985 T ES12704985 T ES 12704985T ES 2573497 T3 ES2573497 T3 ES 2573497T3
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Prior art keywords
piperidine
pyrazine
dihydropyrrolo
spiro
methyl
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ES12704985.6T
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English (en)
Spanish (es)
Inventor
Sara S. Hadida Ruah
Edward Adam Kallel
Mark Thomas Miller
Vijayalaksmi Arumugam
Jason Mccartney
Corey Anderson
Peter Diederik Jan Grootenhuis
Licong JIANG
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C07D471/12Heterocyclic 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
    • 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
    • A61K31/499Spiro-condensed pyrazines or piperazines
    • AHUMAN NECESSITIES
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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • AHUMAN NECESSITIES
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    • A61P9/12Antihypertensives
    • 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
    • C07D471/10Spiro-condensed systems
    • 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
    • C07D471/12Heterocyclic 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
    • C07D471/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
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  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ES12704985.6T 2011-02-02 2012-02-02 Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos Active ES2573497T3 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161438685P 2011-02-02 2011-02-02
US201161438685P 2011-02-02
US201161440987P 2011-02-09 2011-02-09
US201161440987P 2011-02-09
US201161495538P 2011-06-10 2011-06-10
US201161495538P 2011-06-10
PCT/US2012/023593 WO2012106499A1 (en) 2011-02-02 2012-02-02 Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels

Publications (1)

Publication Number Publication Date
ES2573497T3 true ES2573497T3 (es) 2016-06-08

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ID=45689011

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Application Number Title Priority Date Filing Date
ES12704985.6T Active ES2573497T3 (es) 2011-02-02 2012-02-02 Pirrolopirazin-amidas de piperidina espirocíclicas como moduladores de canales iónicos

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Country Link
US (3) US8916565B2 (enExample)
EP (2) EP2670752B1 (enExample)
JP (2) JP6021824B2 (enExample)
KR (1) KR101923367B1 (enExample)
CN (2) CN103403004B (enExample)
AR (1) AR085893A1 (enExample)
AU (1) AU2012212196B2 (enExample)
BR (1) BR112013019211A2 (enExample)
CA (1) CA2825204C (enExample)
CY (1) CY1117471T1 (enExample)
DK (1) DK2670752T3 (enExample)
ES (1) ES2573497T3 (enExample)
HR (1) HRP20160382T8 (enExample)
HU (1) HUE028789T2 (enExample)
IL (1) IL227815B (enExample)
MX (1) MX355907B (enExample)
NZ (1) NZ613028A (enExample)
PL (1) PL2670752T3 (enExample)
PT (1) PT2670752E (enExample)
RS (1) RS54785B1 (enExample)
RU (1) RU2634900C2 (enExample)
SG (1) SG192248A1 (enExample)
SI (1) SI2670752T1 (enExample)
SM (1) SMT201600162B (enExample)
TW (2) TW201604196A (enExample)
WO (1) WO2012106499A1 (enExample)
ZA (1) ZA201305152B (enExample)

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AU2008302598B2 (en) 2007-08-24 2014-07-17 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis
US8598164B2 (en) 2010-05-06 2013-12-03 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
SG192248A1 (en) 2011-02-02 2013-09-30 Vertex Pharma Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels
MX2013009393A (es) 2011-02-18 2013-08-29 Vertex Pharma Piperidinamidas cromano-espirociclicas como moduladores de canales de iones.
US8828996B2 (en) 2011-03-14 2014-09-09 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
CN104024251B (zh) 2011-10-31 2017-08-11 克赛农制药股份有限公司 苯磺酰胺化合物及其作为治疗剂的用途
KR20140105445A (ko) 2011-10-31 2014-09-01 제논 파마슈티칼스 인크. 비아릴 에테르 술폰아미드 및 치료제로서의 그의 용도
JP6038297B2 (ja) 2012-05-22 2016-12-07 ジェネンテック, インコーポレイテッド N−置換ベンズアミドおよび疼痛の処置におけるそれらの使用
JP6309519B2 (ja) 2012-07-06 2018-04-11 ジェネンテック, インコーポレイテッド N置換ベンズアミド及びその使用方法
WO2014022639A1 (en) 2012-08-01 2014-02-06 Vertex Pharmaceuticals Incorporated Solid forms of (4-isopropoxy-3-methoxyphenyl)(2'-methyl-6'-(trifluoromethyl)-3',4'-dihydro-2'h-spiro[piperidine-4,1'-pyrrolo[1,2-a]pyrazine]-1-yl)methanone
US9139529B2 (en) 2013-01-31 2015-09-22 Vertex Pharmaceuticals Incorporated Substituted quinoxalines as sodium channel modulators
IL269964B1 (en) 2013-01-31 2025-09-01 Vertex Pharma Pyridone amide compounds, compositions containing them and uses thereof
EP2961746B1 (en) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物
CN105263490B (zh) 2013-03-14 2018-05-22 基因泰克公司 取代的三唑并吡啶及其使用方法
JP6227112B2 (ja) 2013-03-15 2017-11-08 ジェネンテック, インコーポレイテッド 置換ベンゾオキサゾールとその使用方法
JP6605462B2 (ja) * 2013-07-10 2019-11-13 バーテックス ファーマシューティカルズ インコーポレイテッド イオンチャネルのモジュレーターとしての縮合ピペリジンアミド
SG11201600383SA (en) 2013-07-19 2016-02-26 Vertex Pharma Sulfonamides as modulators of sodium channels
EP3074377B1 (en) 2013-11-27 2018-10-17 Genentech, Inc. Substituted benzamides and methods of use thereof
GEP20207082B (en) 2013-12-13 2020-04-10 Vertex Pharma Prodrugs of pyridone amides useful as modulators of sodium channels
CN106715418A (zh) 2014-07-07 2017-05-24 基因泰克公司 治疗化合物及其使用方法
PE20180575A1 (es) 2015-05-22 2018-04-04 Genentech Inc Benzamidas sustituidas y metodos para utilizarlas
CN108137477A (zh) 2015-08-27 2018-06-08 基因泰克公司 治疗化合物及其使用方法
CR20180242A (es) 2015-09-28 2018-08-10 Genentech Inc Compuestos terapéuticos y sus métodos de uso
EP3380466A1 (en) 2015-11-25 2018-10-03 Genentech, Inc. Substituted benzamides useful as sodium channel blockers
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