EA201071299A1 - 5-[5-[2-(3,5-бис(трифторметил)фенил)-2-метилпропаноилметиламино]-4-(4-фтор-2-метилфенил)]-2-пиридинил-2-алкилпролинамиды в качестве антагонистов рецептора nk1 - Google Patents

5-[5-[2-(3,5-бис(трифторметил)фенил)-2-метилпропаноилметиламино]-4-(4-фтор-2-метилфенил)]-2-пиридинил-2-алкилпролинамиды в качестве антагонистов рецептора nk1

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Publication number
EA201071299A1
EA201071299A1 EA201071299A EA201071299A EA201071299A1 EA 201071299 A1 EA201071299 A1 EA 201071299A1 EA 201071299 A EA201071299 A EA 201071299A EA 201071299 A EA201071299 A EA 201071299A EA 201071299 A1 EA201071299 A1 EA 201071299A1
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EA
Eurasian Patent Office
Prior art keywords
triftoromethyl
methylpropanoylmethylamino
alkylprolinamides
phenil
graduates
Prior art date
Application number
EA201071299A
Other languages
English (en)
Other versions
EA019037B1 (ru
Inventor
Джузеппе Альваро
Агостино Мараско
Original Assignee
Глэксо Уэлкам Мэньюфэкчуринг Пте Лтд.
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.)
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Application filed by Глэксо Уэлкам Мэньюфэкчуринг Пте Лтд. filed Critical Глэксо Уэлкам Мэньюфэкчуринг Пте Лтд.
Publication of EA201071299A1 publication Critical patent/EA201071299A1/ru
Publication of EA019037B1 publication Critical patent/EA019037B1/ru

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    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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Abstract

Изобретение относится к соединению формулы (I) или его фармацевтически приемлемой соли, где R представляет собой C-алкилпригодному для лечения заболеваний и состояний, при которых является полезным антагонизм в отношении рецептора NK1.
EA201071299A 2008-05-14 2009-05-12 5-[5-[2-[3,5-бис(трифторметил)фенил-2-метилпропаноилметиламино]-4-(4-фтор-2-метилфенил)]-2-пиридинил]-2-алкилпролинамиды в качестве антагонистов рецептора nk1 EA019037B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0808747.0A GB0808747D0 (en) 2008-05-14 2008-05-14 Novel compounds
PCT/EP2009/055700 WO2009138393A1 (en) 2008-05-14 2009-05-12 5-[5-[2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanoylmethylamino]-4-(4-fluoro-2-methylphenyl)]-2-pyridinyl-2-alkyl-prolinamide as nk1 receptor antagonists

Publications (2)

Publication Number Publication Date
EA201071299A1 true EA201071299A1 (ru) 2011-06-30
EA019037B1 EA019037B1 (ru) 2013-12-30

Family

ID=39571329

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201071299A EA019037B1 (ru) 2008-05-14 2009-05-12 5-[5-[2-[3,5-бис(трифторметил)фенил-2-метилпропаноилметиламино]-4-(4-фтор-2-метилфенил)]-2-пиридинил]-2-алкилпролинамиды в качестве антагонистов рецептора nk1

Country Status (22)

Country Link
US (4) US20090286836A1 (ru)
EP (1) EP2300452B1 (ru)
JP (1) JP5465716B2 (ru)
KR (1) KR101567116B1 (ru)
CN (1) CN102105458B (ru)
AR (1) AR071721A1 (ru)
AU (1) AU2009248102B8 (ru)
BR (1) BRPI0911990B1 (ru)
CA (1) CA2724219C (ru)
CL (1) CL2009001146A1 (ru)
DK (1) DK2300452T3 (ru)
EA (1) EA019037B1 (ru)
ES (1) ES2446866T3 (ru)
GB (1) GB0808747D0 (ru)
IL (1) IL209197A (ru)
MX (1) MX2010012421A (ru)
PE (1) PE20091847A1 (ru)
PL (1) PL2300452T3 (ru)
TW (1) TWI444376B (ru)
UY (1) UY31824A (ru)
WO (1) WO2009138393A1 (ru)
ZA (1) ZA201007904B (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8426450B1 (en) * 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
JP5806420B1 (ja) 2013-11-08 2015-11-10 キッセイ薬品工業株式会社 カルボキシメチルピペリジン誘導体
TWI649307B (zh) 2014-05-07 2019-02-01 日商橘生藥品工業股份有限公司 Cyclohexylpyridine derivative
WO2016021562A1 (ja) * 2014-08-06 2016-02-11 キッセイ薬品工業株式会社 シアノチオフェン誘導体
WO2018197638A1 (en) 2017-04-27 2018-11-01 Nerre Therapeutics Limited Novel use of (5r)-5-[5-[{2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoyl}(methyl)amino]-4-(4-fluoro-2-methylphenyl)-2-pyridinyl]-2-methyl-d-prolinamide
WO2021154631A1 (en) * 2020-01-30 2021-08-05 Javed Mohammad Combination drug therapies for cns disorders
CA3177477A1 (en) * 2020-06-02 2021-12-09 Nerre Therapeutics Limited Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000050398A2 (en) 1999-02-24 2000-08-31 F. Hoffmann-La Roche Ag Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists
DK1394150T3 (da) 1999-02-24 2011-03-21 Hoffmann La Roche 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister
US6303790B1 (en) 1999-11-29 2001-10-16 Hoffman-La Roche Inc. Process for the preparation of pyridine derivatives
KR100501608B1 (ko) 2000-07-14 2005-07-18 에프. 호프만-라 로슈 아게 4-페닐-피리딘 유도체의 ｎｋ1 수용체의 길항성선구약물로서의 ｎ-산화물
TWI287003B (en) 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
TWI259180B (en) 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
CN100398106C (zh) 2001-04-23 2008-07-02 弗·哈夫曼-拉罗切有限公司 Nk-1受体拮抗剂对抗良性前列腺增生的用途
US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
US6849624B2 (en) 2001-07-31 2005-02-01 Hoffmann-La Roche Inc. Aromatic and heteroaromatic substituted amides
EP1643998B1 (en) 2003-07-03 2007-08-29 F. Hoffmann-La Roche Ag Dual nk1/nk3 antagonists for treating schizophrenia
DE602005026669D1 (de) 2004-07-06 2011-04-14 Hoffmann La Roche Herstellungsverfahren für carboxamid-pyridin-derivate als zwischenprodukte bei der synthese von nk-1-rezeptor-antagonisten
US20060030600A1 (en) * 2004-08-06 2006-02-09 Patrick Schnider Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
DE602006021323D1 (de) * 2005-09-09 2011-05-26 Glaxosmithkline Llc Pyridinderivate und ihre verwendung bei der behandlung psychotischer erkrankungen
US7855218B2 (en) * 2005-10-10 2010-12-21 Convergence Pharmaceuticals Limited Compounds

Also Published As

Publication number Publication date
JP5465716B2 (ja) 2014-04-09
DK2300452T3 (da) 2014-02-17
CN102105458A (zh) 2011-06-22
KR20110017384A (ko) 2011-02-21
AR071721A1 (es) 2010-07-07
US20110060015A1 (en) 2011-03-10
EP2300452B1 (en) 2013-11-20
CL2009001146A1 (es) 2010-09-24
TW201006813A (en) 2010-02-16
PL2300452T3 (pl) 2014-04-30
AU2009248102A1 (en) 2009-11-19
PE20091847A1 (es) 2010-01-09
TWI444376B (zh) 2014-07-11
KR101567116B1 (ko) 2015-11-06
US20130143931A1 (en) 2013-06-06
US8822504B2 (en) 2014-09-02
US20090286836A1 (en) 2009-11-19
EP2300452A1 (en) 2011-03-30
EA019037B1 (ru) 2013-12-30
WO2009138393A1 (en) 2009-11-19
US8344005B2 (en) 2013-01-01
GB0808747D0 (en) 2008-06-18
ZA201007904B (en) 2011-11-30
CN102105458B (zh) 2013-06-12
BRPI0911990B1 (pt) 2021-07-13
CA2724219C (en) 2016-04-05
AU2009248102B8 (en) 2012-07-26
IL209197A0 (en) 2011-01-31
BRPI0911990A2 (pt) 2020-08-18
US9006271B2 (en) 2015-04-14
US20140249188A1 (en) 2014-09-04
UY31824A (es) 2009-11-10
JP2011520834A (ja) 2011-07-21
AU2009248102B2 (en) 2012-06-28
MX2010012421A (es) 2011-03-25
ES2446866T3 (es) 2014-03-10
IL209197A (en) 2014-09-30
CA2724219A1 (en) 2009-11-19

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