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EA201071259A1 - Спиро(пиперидин-4,2-пирролидин)-1-(3,5-трифторметилфенил)метилкарбоксамиды в качестве антагонистов рецептора nk1 тахикинина - Google Patents

Спиро(пиперидин-4,2-пирролидин)-1-(3,5-трифторметилфенил)метилкарбоксамиды в качестве антагонистов рецептора nk1 тахикинина

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Publication number
EA201071259A1
EA201071259A1 EA201071259A EA201071259A EA201071259A1 EA 201071259 A1 EA201071259 A1 EA 201071259A1 EA 201071259 A EA201071259 A EA 201071259A EA 201071259 A EA201071259 A EA 201071259A EA 201071259 A1 EA201071259 A1 EA 201071259A1
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EA
Eurasian Patent Office
Prior art keywords
6alkyl
hydrogen
halogen
independently represent
triftoromethilphenyl
Prior art date
Application number
EA201071259A
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English (en)
Other versions
EA017960B1 (ru
Inventor
Джузеппе Альваро
Эмилиано Кастильони
Агостино Мараско
Original Assignee
Глэксо Уэлкам Мэньюфэкчуринг Пте Лтд.
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Application filed by Глэксо Уэлкам Мэньюфэкчуринг Пте Лтд. filed Critical Глэксо Уэлкам Мэньюфэкчуринг Пте Лтд.
Publication of EA201071259A1 publication Critical patent/EA201071259A1/ru
Publication of EA017960B1 publication Critical patent/EA017960B1/ru

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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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Abstract

Соединения формулы (I) или его фармацевтически приемлемая сольгде R представляет собой водород или Салкил; R1 представляет собой водород, Салкил, С(О)ОН, C(O)NHили (Салкилен)R10; R2 и R3 независимо представляют собой водород, Салкил или R2 вместе с R3 и вместе с атомом углерода, к которому они присоединены, образуют Сциклоалкильную группу; R4 представляет собой Салкил, Салкокси или галоген; R5 и R7 независимо представляют собой водород, гидрокси, галоген, C(O)NH, С(О)ОН или (Салкилен)R10; R6 и R8 независимо представляют собой водород или галоген; R9 представляет собой водород, (Салкилен)R10, C(O)NH, С(О)ОН или R9 вместе с R образуют 6-членное гетероциклическое кольцо, необязательно содержащее, кроме того, гетероатом, выбранный из кислорода, серы или азота; R10 представляет собой водород, галоген, гидрокси, C(O)NH, C(O)NH(Салкил), С(О)N(Салкил)или С(О)ОН; n равно 0, 1 или 2; способы их получения, содержащие их композиции и их применение при лечении заболеваний и состояний, при которых полезным является антагонизм NK1.
EA201071259A 2008-05-01 2009-04-29 Производные 1,8-диазоспиро[4,5]декан-8-карбоксамида, обладающие антагонистической активностью в отношении рецептора nk1 EA017960B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0808030.1A GB0808030D0 (en) 2008-05-01 2008-05-01 Novel compounds
PCT/EP2009/055190 WO2009133135A1 (en) 2008-05-01 2009-04-29 Spiro (piperidine-4, 2 ' -pyrrolidine) -1- (3, 5- trifluoromethyl phenyl) methylcarboxamides as nk1 tachikynin receptor antagonists

Publications (2)

Publication Number Publication Date
EA201071259A1 true EA201071259A1 (ru) 2011-10-31
EA017960B1 EA017960B1 (ru) 2013-04-30

Family

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EA201071259A EA017960B1 (ru) 2008-05-01 2009-04-29 Производные 1,8-диазоспиро[4,5]декан-8-карбоксамида, обладающие антагонистической активностью в отношении рецептора nk1

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US (2) US8367692B2 (ru)
EP (1) EP2300474B1 (ru)
JP (1) JP5524183B2 (ru)
KR (1) KR101645743B1 (ru)
CN (1) CN102083832B (ru)
AU (1) AU2009242120B2 (ru)
BR (1) BRPI0910530B8 (ru)
CA (1) CA2723062C (ru)
CY (1) CY1113458T1 (ru)
DK (1) DK2300474T3 (ru)
EA (1) EA017960B1 (ru)
ES (1) ES2395571T3 (ru)
GB (1) GB0808030D0 (ru)
HR (1) HRP20121018T1 (ru)
IL (1) IL208917A (ru)
MX (1) MX2010011985A (ru)
PL (1) PL2300474T3 (ru)
PT (1) PT2300474E (ru)
RS (1) RS52719B (ru)
SI (1) SI2300474T1 (ru)
WO (1) WO2009133135A1 (ru)
ZA (1) ZA201007519B (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2484674A1 (en) 2011-02-02 2012-08-08 Rottapharm S.P.A. Spiro aminic compounds with NK1 antagonist activity
CN109651368A (zh) * 2018-12-17 2019-04-19 武汉药明康德新药开发有限公司 4-甲酸甲酯-2-氧-1,8-二氮杂螺[4.5]癸烷-8-甲酸叔丁酯的制备方法
IL298589A (en) * 2020-06-02 2023-01-01 Nerre Therapeutics Ltd Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9215706D0 (en) 1992-07-23 1992-09-09 Tollpass Limited Parking toll collecting system
EP0702681A1 (en) 1993-06-07 1996-03-27 Merck & Co. Inc. Spiro-substituted azacycles as neurokinin antagonists
US6274604B1 (en) 1996-07-17 2001-08-14 Merck & Co., Inc. Alteration of circadian rhythmicity with a tachykinin antagonist
US6013652A (en) 1997-12-04 2000-01-11 Merck & Co., Inc. Spiro-substituted azacycles as neurokinin antagonists
WO2001030348A1 (en) 1999-10-25 2001-05-03 Janssen Pharmaceutica N.V. Use of substance p antagonists for influencing the circadian timing system
US7482365B2 (en) * 2002-02-08 2009-01-27 Glaxo Group Limited Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases
GB0203022D0 (en) * 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
JP4389478B2 (ja) * 2002-05-29 2009-12-24 田辺三菱製薬株式会社 新規ピペリジン誘導体
JP4380508B2 (ja) * 2003-11-28 2009-12-09 田辺三菱製薬株式会社 医薬組成物
JP2005154380A (ja) * 2003-11-28 2005-06-16 Tanabe Seiyaku Co Ltd ピペリジン誘導体
US7390905B2 (en) * 2003-11-28 2008-06-24 Mitsubishi Tanabe Pharma Corporation Piperidine compound and process for preparing the same
GB0514707D0 (en) * 2005-07-18 2005-08-24 Glaxo Group Ltd Chemical compounds

Also Published As

Publication number Publication date
CN102083832B (zh) 2013-06-05
PL2300474T3 (pl) 2013-03-29
ES2395571T3 (es) 2013-02-13
EP2300474A1 (en) 2011-03-30
US8633214B2 (en) 2014-01-21
DK2300474T3 (da) 2012-12-10
JP2011518861A (ja) 2011-06-30
BRPI0910530A2 (pt) 2015-08-18
IL208917A (en) 2014-06-30
MX2010011985A (es) 2011-02-24
US20110053922A1 (en) 2011-03-03
WO2009133135A1 (en) 2009-11-05
KR101645743B1 (ko) 2016-08-04
IL208917A0 (en) 2011-01-31
US20130123250A1 (en) 2013-05-16
EP2300474B1 (en) 2012-10-03
PT2300474E (pt) 2013-01-07
SI2300474T1 (sl) 2013-01-31
KR20110015421A (ko) 2011-02-15
ZA201007519B (en) 2011-11-30
GB0808030D0 (en) 2008-06-11
CA2723062A1 (en) 2009-11-05
CA2723062C (en) 2016-07-05
BRPI0910530B1 (pt) 2020-02-11
RS52719B (en) 2013-08-30
CY1113458T1 (el) 2016-06-22
JP5524183B2 (ja) 2014-06-18
HRP20121018T1 (hr) 2013-01-31
BRPI0910530B8 (pt) 2021-05-25
US8367692B2 (en) 2013-02-05
AU2009242120A1 (en) 2009-11-05
CN102083832A (zh) 2011-06-01
EA017960B1 (ru) 2013-04-30
AU2009242120B2 (en) 2012-05-24

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