BR9813381A - "derivados de imidazol substituìdo possuindo atividade semelhante a agonista em receptores adrenérgicos alfa 2b ou 2b/2c" - Google Patents

"derivados de imidazol substituìdo possuindo atividade semelhante a agonista em receptores adrenérgicos alfa 2b ou 2b/2c"

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Publication number
BR9813381A
BR9813381A BR9813381-0A BR9813381A BR9813381A BR 9813381 A BR9813381 A BR 9813381A BR 9813381 A BR9813381 A BR 9813381A BR 9813381 A BR9813381 A BR 9813381A
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Brazil
Prior art keywords
alpha
integer
attached
lower alkyl
activity
Prior art date
Application number
BR9813381-0A
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English (en)
Inventor
Ken Chow
Daniel W Gil
James A Burke
Dale A Harcourt
Michael E Garst
Larry A Wheeler
Stephen A Munk
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Allergan Sales Inc
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Publication date
Application filed by Allergan Sales Inc filed Critical Allergan Sales Inc
Publication of BR9813381A publication Critical patent/BR9813381A/pt

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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/06—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/84—Sulfur atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/28—Nitrogen atoms not forming part of a nitro radical
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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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

Patente de Invenção: <B>"DERIVADOS DE IMIDAZOL SUBSTITUìDO POSSUINDO ATIVIDADE SEMELHANTE A AGONISTA EM RECEPTORES ADRENéRGICOS ALFA 2B OU 2B/2C"<D>. Compostos possuindo atividade adrenérgica que são agonistas seletivos para um ou ambos os subtipos alfa 2B ou alfa 2C receptores adrenoceptores em preferência ao subtipo alfa 2A receptor adrenoceptor; o composto ativo sendo selecionado dos compostos possuindo a fórmula (I) onde linhas as pontilhadas representam ligações opcionais; contanto que duas ligações duplas não possam compartilhar um átomo de carbono comum; R é H ou alquila inferior; X é S ou C(H)R¹, onde R¹ e H ou alquila inferior, porém R¹ está ausente quando a ligação entre X e o anel representado pela fórmula (a) for uma ligação dupla; Y é O, N, S, (CR¹2)~ y~, onde y é um número inteiro de cerca de 1 a 3, -CH=CH- ou Y¹CH~ 2~, onde Y¹ é O, N ou S; x é um número inteiro de 1 ou 2, onde x é 1 quando R², R³ ou R^ 4^ for ligado a um átomo de carbono não saturado e x é 2 quando R², R³ ou R^ 4^ for ligado a um átomo de carbono saturado; R² é H, alquila inferior, halogênio, hidróxi ou alcóxi inferior, ou, quando anexado a um átomo de carbono saturado, R~ 2~ pode ser oxo; R~ 3~ e R~ 4~ são, cada um, H alquila inferior, hidróxi, alcóxi inferior, ou fenila ou, em conjunto, são -(C(R²)x)z-; -Y¹(C(R²)x)z'-; - Y¹(C(R²)x)y Y¹-; -(C(R²)x)- Y¹-(C(R²)x)-; - (C(R²)X)- Y¹ (C(R²)x)-(C(R²)x)- e - Y¹-(C(R²)x)- Y¹-(C(R²)x)- onde z é um número inteiro de cerca de 3 to 5, z' é um número inteiro de cerca de 2 a 4 e x e y são conforme definidos acima, e adicionalmente tanto a extremidade de cada uma destas porções divalentes pode ser anexada tanto a R³ quanto R^ 4^ para formar uma estrutura de anel condensada e os anéis formados podem ser totalmente insaturados, parcialmente insaturados, ou totalmente saturados; e sendo útil para tratamento de espasticidade muscular incluindo micturição hiperativa, diarréia, diurese, síndromes de ausência, dor incluindo dor neuropática, doenças neurodegenerativas, deficiência de memória e cognição, psicoses incluindo distúrbios maníacos e ansiedade, hipertensão, isquemia cardíaca falha cardíaca congestiva, e congestão nasal, sem os efeitos colaterais de sedação ou cardiovasculares.
BR9813381-0A 1997-12-04 1998-12-03 "derivados de imidazol substituìdo possuindo atividade semelhante a agonista em receptores adrenérgicos alfa 2b ou 2b/2c" BR9813381A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US98534797A 1997-12-04 1997-12-04
PCT/US1998/025669 WO1999028300A1 (en) 1997-12-04 1998-12-03 Substituted imidazole derivatives having agonist-like activity at alpha 2b or 2b/2c adrenergic receptors

Publications (1)

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BR9813381A true BR9813381A (pt) 2000-10-03

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BR9813381-0A BR9813381A (pt) 1997-12-04 1998-12-03 "derivados de imidazol substituìdo possuindo atividade semelhante a agonista em receptores adrenérgicos alfa 2b ou 2b/2c"

Country Status (22)

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EP (2) EP1036065B1 (pt)
JP (3) JP4783502B2 (pt)
KR (1) KR100544787B1 (pt)
CN (1) CN1284066A (pt)
AR (1) AR017807A1 (pt)
AT (1) ATE266643T1 (pt)
AU (1) AU744798B2 (pt)
BR (1) BR9813381A (pt)
CA (1) CA2312334A1 (pt)
DE (1) DE69823868T2 (pt)
DK (1) DK1036065T3 (pt)
ES (1) ES2216339T3 (pt)
HU (1) HUP0004557A3 (pt)
IL (2) IL136388A0 (pt)
NO (2) NO317292B1 (pt)
NZ (1) NZ504667A (pt)
PL (1) PL341009A1 (pt)
PT (1) PT1036065E (pt)
RU (1) RU2235092C2 (pt)
SK (1) SK8542000A3 (pt)
TW (1) TW577878B (pt)
WO (1) WO1999028300A1 (pt)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002254265B2 (en) * 1997-12-04 2008-05-15 Allergan, Inc. Imidiazole derivatives and their use as agonists selective at alpha 2B or 2B/2C adrenergic receptors
ATE266643T1 (de) * 1997-12-04 2004-05-15 Allergan Inc Substituierte imidazole derivate mit agonistischähnlicher wirkung auf die alpha 2b oder 2b/2c adrenergischen rezeptoren
US6841684B2 (en) * 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
TWI283669B (en) * 1999-06-10 2007-07-11 Allergan Inc Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B/2C adrenergic receptors
FI20000073A0 (fi) * 2000-01-14 2000-01-14 Orion Yhtymae Oy Uusia imidatsolijohdannaisia
US6388090B2 (en) 2000-01-14 2002-05-14 Orion Corporation Imidazole derivatives
US6294553B1 (en) * 2000-02-15 2001-09-25 Allergan Sales, Inc. Method for treating ocular pain
US6593324B2 (en) 2000-03-01 2003-07-15 Orion Corporation Dervatives of quinoline as alpha-2 antagonists
JP2006036636A (ja) * 2000-11-22 2006-02-09 Nippon Shinyaku Co Ltd 消化管機能障害治療剤及びスクリーニング方法
NZ535950A (en) 2002-04-03 2007-11-30 Orion Corp Polycyclic compounds as potent alpha2-adrenoceptor antagonists
WO2003088992A1 (fr) * 2002-04-22 2003-10-30 Takeda Chemical Industries, Ltd. Nouvelle methode de criblage
US7091232B2 (en) 2002-05-21 2006-08-15 Allergan, Inc. 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
US7276522B2 (en) 2002-05-21 2007-10-02 Allergan, Inc. 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones, 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
US7358269B2 (en) 2002-05-21 2008-04-15 Allergan, Inc. 2-((2-Thioxo-2,3-dihydro-1H-imidazol-4-yl)methyl)-3,4-dihydronapthalen-1(2H)-one
US7345065B2 (en) 2002-05-21 2008-03-18 Allergan, Inc. Methods and compositions for alleviating pain
US7323485B2 (en) 2002-05-21 2008-01-29 Allergan, Inc. 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
ATE380551T1 (de) * 2002-10-08 2007-12-15 Allergan Inc Verwendung von brimonidine zur behandlung von dementia und morbus parkinson
MXPA05003664A (es) * 2002-10-08 2005-06-08 Allergan Inc Agonistas del adrenoceptor alfa 2b o 2b/2c para tratamiento de neurodegeneracion.
AU2005287038B2 (en) 2004-09-20 2012-02-02 Janssen Pharmaceutica N.V. Novel tetracyclic heteroatom containing derivatives useful as sex steroid hormone receptor modulators
PL1796664T3 (pl) 2004-09-20 2014-04-30 Janssen Pharmaceutica Nv Nowe, zawierające heteroatom, pochodne tetracykliczne użyteczne jako modulatory receptora steroidowego hormonu płci
WO2006036497A2 (en) * 2004-09-24 2006-04-06 Allergan, Inc. 4-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
CA2581828A1 (en) 2004-09-24 2006-04-06 Allergan, Inc. 4-(heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
JP4986856B2 (ja) * 2004-09-28 2012-07-25 アラーガン、インコーポレイテッド 特異的または選択的α２アドレナリン作動剤としての不置換および置換４−ベンジル−１，３−ジヒドロ−イミダゾール−２−チオンならびにその使用方法
US7390829B2 (en) 2005-06-29 2008-06-24 Allergan, Inc. Alpha-2 adrenergic agonists
US7700592B2 (en) 2005-08-25 2010-04-20 Schering Corporation α2C adrenoreceptor agonists
RU2008110902A (ru) * 2005-08-25 2009-09-27 Шеринг Корпорейшн (US) Агонисты адренорецепторов альфа а2с
US7592362B2 (en) 2006-01-19 2009-09-22 Pfizer Limited Substituted imidazoles
ES2338716T3 (es) * 2006-01-27 2010-05-11 F.Hoffmann-La Roche Ag Uso de derivados de 4-imidazol para trastornos del snc.
EA200870452A1 (ru) * 2006-04-20 2009-04-28 Янссен Фармацевтика Н.В. Производные замещенного пиразинона для применения в качестве лекарственных средств
US20090281099A1 (en) * 2006-05-22 2009-11-12 Andres-Gil Jose Ignacio Substituted pyrazinone derivatives for use as a medicine
AU2007312390B2 (en) 2006-10-19 2013-03-28 F. Hoffmann-La Roche Ag Aminomethyl-4-imidazoles
ATE533755T1 (de) 2006-11-02 2011-12-15 Hoffmann La Roche Substituierte 2-imidazole als modulatoren der mit spurenaminen assoziierten rezeptoren
WO2008058867A2 (en) * 2006-11-16 2008-05-22 F. Hoffmann-La Roche Ag Substituted 4-imidazoles
CN101190218B (zh) * 2006-11-20 2010-12-22 四川科瑞德制药有限公司 替扎尼定及其衍生物在制备抗焦虑症药物中的用途
ATE509628T1 (de) 2006-12-13 2011-06-15 Hoffmann La Roche Neue 2-imidazole als liganden für trace amine associated receptors (taar)
US20080146523A1 (en) 2006-12-18 2008-06-19 Guido Galley Imidazole derivatives
US7868020B2 (en) 2007-01-12 2011-01-11 Allergan, Inc. Quinolynylmethylimidizoles as therapeutic agents
US8119807B2 (en) 2007-01-12 2012-02-21 Allergan, Inc. Quinolynylmethylimidizoles as therapeutic agents
WO2008086131A1 (en) 2007-01-12 2008-07-17 Allergan, Inc. Naphthylmethylimidizoles as therapeutic agents
EP2114906B1 (en) 2007-02-02 2014-08-06 F. Hoffmann-La Roche AG 2-aminooxazolines as taar1 ligands for cns disorders
RU2009134059A (ru) 2007-02-13 2011-03-20 Шеринг Корпорейшн (US) Функционально селективные агонисты альфа2с адренорецептора
CN101657429A (zh) 2007-02-13 2010-02-24 先灵公司 功能选择性α2C肾上腺素能受体激动剂
JP2010518161A (ja) 2007-02-13 2010-05-27 シェーリング コーポレイション 機能選択性α２Ｃアドレナリン受容体アゴニストとしてのクロマン誘導体および類似体
CA2676944C (en) 2007-02-15 2016-01-19 F. Hoffmann-La Roche Ag 2-aminooxazolines as taar1 ligands
EP2160386B1 (en) * 2007-05-23 2012-07-11 Allergan, Inc. Therapeutic ((phenyl)imidazolyl)methylquinolinyl compounds
CN101318020B (zh) * 2007-06-06 2011-09-28 四川科瑞德制药有限公司 抗焦虑或/和抗抑郁的药物组合物及用途
MX2009013742A (es) 2007-07-02 2010-01-26 Hoffmann La Roche 2-imidazolinas.
EP2173719A1 (en) 2007-07-03 2010-04-14 F. Hoffmann-Roche AG 4-imidazolines and their use as antidepressants
CN101778628B (zh) * 2007-07-17 2013-02-06 阿勒根公司 治疗焦虑的方法
TWI457122B (zh) 2007-07-20 2014-10-21 Orion Corp 作為用於治療周邊和中央神經系統疾病之alpha2C拮抗劑的2,3－二氫苯並[1,4]戴奧辛－2－基甲基衍生物
AU2008281918A1 (en) 2007-07-27 2009-02-05 F. Hoffmann-La Roche Ag 2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as TAAR-ligands
EP2185502A1 (en) 2007-08-03 2010-05-19 F. Hoffmann-Roche AG Pyridinecarboxamide and benzamide derivatives as taar1 ligands
WO2009020578A1 (en) * 2007-08-06 2009-02-12 Schering Corporation Alpha2c adrenoreceptor agonists
US7902247B2 (en) 2008-01-09 2011-03-08 Allergan, Inc. Substituted-aryl-2-phenylethyl-1H-imidazole compounds as subtype selective modulators of alpha 2B and/or alpha 2C adrenergic receptors
WO2009091735A1 (en) * 2008-01-18 2009-07-23 Allergan.Inc Substitued-aryl-(imidazole)-methyl)-phenyl compounds as subtype selective modulators of alpha 2b and/or alpha 2c adrenergic receptors
WO2009105504A2 (en) 2008-02-21 2009-08-27 Schering Corporation Functionally selective alpha2c adrenoreceptor agonists
CA2724293A1 (en) * 2008-05-13 2009-11-19 Allergan, Inc. Quinolynylmethylimidizoles as therapeutic agents
DE102008001932A1 (de) 2008-05-21 2009-11-26 Bayer Cropscience Ag Substiuierte Spiroisoxazoline
US8242153B2 (en) 2008-07-24 2012-08-14 Hoffmann-La Roche Inc. 4,5-dihydro-oxazol-2YL derivatives
EP2356106A1 (en) 2008-10-07 2011-08-17 Schering Corporation Biaryl spiroaminooxazoline analogues as alpha2c adrenergic receptor modulators
US8354441B2 (en) 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
US9452980B2 (en) 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
EP3093017B1 (en) * 2010-11-16 2021-01-06 Allergan, Inc. Pharmaceutical composition comprising (s)-(3-(1-(1h-imidazol-4-yl)ethyl)-2-methylphenyl)methanol for treating optic neuropathy
US9073911B2 (en) 2011-06-09 2015-07-07 Hoffmann-La Roche Inc. Pyrazole derivatives
US9029370B2 (en) 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
US9095576B2 (en) 2011-11-21 2015-08-04 Allergan, Inc. Pharmaceutical compositions comprising 4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole derivatives for treating retinal diseases
AR090557A1 (es) * 2012-04-02 2014-11-19 Orion Corp DERIVADOS IMIDAZOLICOS AGONISTAS ADRENERGICOS a2
EP3757102A1 (en) 2016-03-17 2020-12-30 F. Hoffmann-La Roche AG 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar
CN110240542B (zh) * 2019-06-24 2020-05-12 牡丹江医学院 一种选择性β1-肾上腺素受体抑制剂及其在制备心血管疾病药物中的用途
WO2023067518A1 (en) * 2021-10-20 2023-04-27 Assembly Biosciences, Inc. Process

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU85747A1 (fr) * 1985-01-28 1986-08-04 Continental Pharma Derives d'imidazole leur preparation et utilisation ainsi que les compositions pharmaceutiques contenant des derives
FI864570A0 (fi) * 1986-11-11 1986-11-11 Farmos Oy Terapeutiskt anvaendbar foerening.
US4882343A (en) * 1987-08-28 1989-11-21 G. D. Searle & Co. Biarylalkylimidazole derivatives as anti-depressants
JPH01242571A (ja) * 1988-03-22 1989-09-27 Mitsui Petrochem Ind Ltd イミダゾール誘導体の製造方法
GB8823980D0 (en) * 1988-10-13 1988-11-23 Glaxo Group Ltd Chemical compounds
WO1993012107A1 (en) * 1991-12-18 1993-06-24 Schering Corporation Imidazoylalkyl substituted with a six membered nitrogen containing heterocyclic ring
AU5118493A (en) * 1992-10-06 1994-04-26 Tokyo Tanabe Company Limited Aromatase inhibitor
CA2220517A1 (en) * 1995-05-12 1996-11-14 Allergan Aryl-imidazolines and aryl-imidazoles useful as alpha-2 adrenergic agonists without cardiovascular side effects
GB9520150D0 (en) * 1995-10-03 1995-12-06 Orion Yhtymae Oy New imidazole derivatives
US5621113A (en) * 1996-03-28 1997-04-15 Ortho Pharmaceutical Corporation 4-[(thien-2-yl)methyl]-imidazole analgesics
US5750720A (en) * 1996-03-28 1998-05-12 Ortho Pharmaceutical Corporation 4- (thien-3-yl)methyl!-imidazole analgesics
US6841684B2 (en) * 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
ATE266643T1 (de) * 1997-12-04 2004-05-15 Allergan Inc Substituierte imidazole derivate mit agonistischähnlicher wirkung auf die alpha 2b oder 2b/2c adrenergischen rezeptoren

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