EA201170130A1 - Бензоксазины, бензотиазины и родственные соединения, обладающие ингибирующей nos активностью - Google Patents

Бензоксазины, бензотиазины и родственные соединения, обладающие ингибирующей nos активностью

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Publication number
EA201170130A1
EA201170130A1 EA201170130A EA201170130A EA201170130A1 EA 201170130 A1 EA201170130 A1 EA 201170130A1 EA 201170130 A EA201170130 A EA 201170130A EA 201170130 A EA201170130 A EA 201170130A EA 201170130 A1 EA201170130 A1 EA 201170130A1
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Eurasian Patent Office
Prior art keywords
nhc
optionally substituted
alkyl
alkoxy
benzothiazines
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EA201170130A
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English (en)
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EA021798B1 (ru
Inventor
Джайлялль Рамно
Субхаш К. Аннеди
Сара Силверман
Питер Дав
Шон Мэддафорд
Суман Ракхит
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Ньюрэксон, Инк.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41465440&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201170130(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ньюрэксон, Инк. filed Critical Ньюрэксон, Инк.
Publication of EA201170130A1 publication Critical patent/EA201170130A1/ru
Publication of EA021798B1 publication Critical patent/EA021798B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
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  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Rheumatology (AREA)
  • Addiction (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Описаны бензоксазины и бензотиазины формулы (I), в которой Q представляет собой О-(CHR)или S-(CHR); Rи каждый Rпредставляют собой Н, необязательно замещенный [Cалкил, Салкарил, Салкгетероциклил, Cгетероциклил, Сциклоалкил, Салкциклоалкил] или -(CRR)NRR, где R, R, R, Rпредставляют собой независимо водород, необязательно замещенный [Cалкил, Cалкарил, Салкгетероциклил, Сгетероциклил, Сциклоалкил и т.д.] или где Rи Rобъединяются с образованием =O, или где Rи Rобъединяются с образованием необязательно замещенного Сгетероциклила и n равно целому числу 1-6; каждый из Rи Rпредставляет собой Н, галоген, необязательно замещенный [C-алкил, Сарил, Cалкарил, Сгетероциклил, Cалкокси, Cтиоалкокси, (СН)NHC(NH)R, (СН)NHC(S)NHR, C-алкгетероциклил] или гидрокси, где r2 равно целому числу от 0 до 2, Rпредставляет собой необязательно замещенный [Cалкил, Сарил, Салкарил, Сгетероциклил, Салкгетероциклил, Cтиоалкокси, Стиоалкарил, арилоил, Стиоалкгетероциклил или амино]; каждый из Rи Rпредставляет собой Н, галоген, (CH)NHC(NH)Rили (CH)NHC(S)NHR; Yи Yвместе обозначают =O, или Yи Yпредставляют собой независимо Н, необязательно замещенный [Cалкил, Сарил, Cалкарил, Сгетероциклил, Cалкокси, Cтиоалкокси, Салкгетероциклил] или гидрокси; где только один из R, R, Rи Rпредставляет собой (CH)NHC(NH)Rили (CH)NHC(S)NHR; или их фармацевтически приемлемые соли или пролекарства. Указанные бензоксазины и бензотиазины формулы (I) ингибируют (оксид азота)-синтазу (NOS), особенно селективно ингибируют нейронную (оксид азота)-синтазу (nNOS), предпочтительно относительно других изоформ NOS. Ингибиторы NOS формулы (I), отдельно или в комбинации с другими фармацевтически активными агентами, можно применять для лечения или предупреждения различных патологических состояний.
EA201170130A 2008-07-03 2009-07-03 Бензоксазины, бензотиазины и родственные соединения, обладающие ингибирующей nos активностью EA021798B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13388708P 2008-07-03 2008-07-03
PCT/CA2009/000923 WO2010000073A1 (en) 2008-07-03 2009-07-03 Benzoxazines, benzothiazines, and related compounds having nos inhibitory activity

Publications (2)

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EA201170130A1 true EA201170130A1 (ru) 2011-08-30
EA021798B1 EA021798B1 (ru) 2015-09-30

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US (3) US8106043B2 (ru)
EP (1) EP2310386A4 (ru)
JP (1) JP5572157B2 (ru)
KR (1) KR20110036607A (ru)
CN (1) CN102143961B (ru)
AR (1) AR072471A1 (ru)
AU (1) AU2009266386B2 (ru)
BR (1) BRPI0913915A2 (ru)
CA (1) CA2729246C (ru)
CL (1) CL2010001633A1 (ru)
EA (1) EA021798B1 (ru)
IL (1) IL210195A (ru)
MX (1) MX2011000124A (ru)
MY (1) MY158796A (ru)
NZ (1) NZ590727A (ru)
SG (1) SG192470A1 (ru)
TW (1) TWI458726B (ru)
UA (1) UA105182C2 (ru)
WO (1) WO2010000073A1 (ru)
ZA (1) ZA201100436B (ru)

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WO2010000073A1 (en) 2010-01-07
AR072471A1 (es) 2010-09-01
BRPI0913915A2 (pt) 2015-10-13
AU2009266386B2 (en) 2015-02-19
TWI458726B (zh) 2014-11-01
CA2729246C (en) 2018-08-21
JP2011526251A (ja) 2011-10-06
US8618286B2 (en) 2013-12-31
CL2010001633A1 (es) 2011-05-20
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IL210195A (en) 2015-08-31
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CA2729246A1 (en) 2010-01-07
AU2009266386A1 (en) 2010-01-07
MY158796A (en) 2016-11-15
EA021798B1 (ru) 2015-09-30
UA105182C2 (ru) 2014-04-25
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IL210195A0 (en) 2011-03-31

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