BRPI0910530B8 - compostos espiro (piperidina-4,2’-pirrolideno)-1-(3,5-trifluormetilfenil)metilcarboxamidas, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para o tratamento de depressão, ansiedade, distúrbios do sono ou êmese - Google Patents

compostos espiro (piperidina-4,2’-pirrolideno)-1-(3,5-trifluormetilfenil)metilcarboxamidas, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para o tratamento de depressão, ansiedade, distúrbios do sono ou êmese

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Publication number
BRPI0910530B8
BRPI0910530B8 BRPI0910530A BRPI0910530A BRPI0910530B8 BR PI0910530 B8 BRPI0910530 B8 BR PI0910530B8 BR PI0910530 A BRPI0910530 A BR PI0910530A BR PI0910530 A BRPI0910530 A BR PI0910530A BR PI0910530 B8 BRPI0910530 B8 BR PI0910530B8
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BR
Brazil
Prior art keywords
alkyl
compounds
hydrogen
halogen
methylcarboxamides
Prior art date
Application number
BRPI0910530A
Other languages
English (en)
Inventor
Marasco Agostino
Castiglioni Emiliano
Alvaro Giuseppe
Original Assignee
Glaxo Wellcome Mfg Pte Ltd
Nerre Therapeutics Ltd
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 Glaxo Wellcome Mfg Pte Ltd, Nerre Therapeutics Ltd filed Critical Glaxo Wellcome Mfg Pte Ltd
Publication of BRPI0910530A2 publication Critical patent/BRPI0910530A2/pt
Publication of BRPI0910530B1 publication Critical patent/BRPI0910530B1/pt
Publication of BRPI0910530B8 publication Critical patent/BRPI0910530B8/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
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  • Neurology (AREA)
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  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
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  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

espiro (piperidina-4, 2' -pirrolideno) -1- (3, 5- trifluormetilfenil) metilcarboxamidas como antagonistas do receptor de taquicinina nk1. são revelados compostos da fórmula (i) ou um sal farmaceuticamente aceitável destes em que r é hidrogênio ou alquila c 1-4; r1 é hidrogênio, alquila c 1-4, c(o)oh, c(o)nh2 ou (alquileno c 1-4)r10; r2 e r3 são independentemente hidrogênio, alquila c 1-4 ou r2 junto com r3 e junto com o átomo de carbono ao qual eles são anexados formam um grupo cicloalquila c3-8; r4 é alquila c 1-4, alcóxi c 1-4 ou halogênio; r5 e r7 são independentemente hidrogênio, hidróxi, halogênio, c(o)nh2, c(o)oh ou (alquileno c 1-4) r10; r6 e r8 são independentemente hidrogênio ou halogênio; r9 é hidrogênio, (alquileno c 1-4)r10, c(o)nh2, c(o)oh ou r9 junto com r formam um anel heterocíclico de 6 membros opcionalmente contendo um heteroátomo selecionado adicionalmente de oxigênio, enxofre ou nitrogênio; r10 é hidrogênio, halogênio hidróxi, c(o)nh2, c(o)nh(alquila c 1-4), c(o)n(alquil c 1-4)2 ou c(o)oh; n é 0, 1 ou 2, processos para sua preparação, a composições contendo-os e a seu uso no tratamento de doenças e condições para qual o antagonismo de nk1 é benéfico.
BRPI0910530A 2008-05-01 2009-04-29 compostos espiro (piperidina-4,2’-pirrolideno)-1-(3,5-trifluormetilfenil)metilcarboxamidas, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para o tratamento de depressão, ansiedade, distúrbios do sono ou êmese BRPI0910530B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0808030.1A GB0808030D0 (en) 2008-05-01 2008-05-01 Novel compounds
GB0808030.1 2008-05-01
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 (3)

Publication Number Publication Date
BRPI0910530A2 BRPI0910530A2 (pt) 2015-08-18
BRPI0910530B1 BRPI0910530B1 (pt) 2020-02-11
BRPI0910530B8 true BRPI0910530B8 (pt) 2021-05-25

Family

ID=39537192

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0910530A BRPI0910530B8 (pt) 2008-05-01 2009-04-29 compostos espiro (piperidina-4,2’-pirrolideno)-1-(3,5-trifluormetilfenil)metilcarboxamidas, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para o tratamento de depressão, ansiedade, distúrbios do sono ou êmese

Country Status (22)

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

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
MX2022014901A (es) 2020-06-02 2023-01-18 Nerre Therapeutics Ltd Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones.

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
EP0912174B1 (en) 1996-07-17 2004-04-28 MERCK & CO., INC. Alteration of circadian rhythmicity with non-peptidal neurikinin-1 receptor antagonists
US6013652A (en) 1997-12-04 2000-01-11 Merck & Co., Inc. Spiro-substituted azacycles as neurokinin antagonists
AU7788500A (en) 1999-10-25 2001-05-08 Janssen Pharmaceutica N.V. Use of substance p antagonists for influencing the circadian timing system
JP2005522436A (ja) * 2002-02-08 2005-07-28 グラクソ　グループ　リミテッド ピペリジルカルボキシアミド誘導体またはそのタキキニン介在疾患の治療における使用
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
KR100877641B1 (ko) * 2003-11-28 2009-01-09 미쓰비시 타나베 파마 코퍼레이션 피페리딘 화합물 및 그의 제조 방법
GB0514707D0 (en) * 2005-07-18 2005-08-24 Glaxo Group Ltd Chemical compounds

Also Published As

Publication number Publication date
PT2300474E (pt) 2013-01-07
US20130123250A1 (en) 2013-05-16
CY1113458T1 (el) 2016-06-22
EA201071259A1 (ru) 2011-10-31
AU2009242120B2 (en) 2012-05-24
BRPI0910530A2 (pt) 2015-08-18
SI2300474T1 (sl) 2013-01-31
US8367692B2 (en) 2013-02-05
EP2300474B1 (en) 2012-10-03
PL2300474T3 (pl) 2013-03-29
US8633214B2 (en) 2014-01-21
CA2723062C (en) 2016-07-05
WO2009133135A1 (en) 2009-11-05
JP5524183B2 (ja) 2014-06-18
JP2011518861A (ja) 2011-06-30
KR20110015421A (ko) 2011-02-15
HRP20121018T1 (hr) 2013-01-31
MX2010011985A (es) 2011-02-24
ZA201007519B (en) 2011-11-30
KR101645743B1 (ko) 2016-08-04
IL208917A (en) 2014-06-30
EA017960B1 (ru) 2013-04-30
EP2300474A1 (en) 2011-03-30
CA2723062A1 (en) 2009-11-05
GB0808030D0 (en) 2008-06-11
US20110053922A1 (en) 2011-03-03
IL208917A0 (en) 2011-01-31
BRPI0910530B1 (pt) 2020-02-11
ES2395571T3 (es) 2013-02-13
CN102083832B (zh) 2013-06-05
RS52719B (sr) 2013-08-30
DK2300474T3 (da) 2012-12-10
AU2009242120A1 (en) 2009-11-05
CN102083832A (zh) 2011-06-01

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