CA2986083A1 - Efflux-pump inhibitors and therapeutic uses thereof - Google Patents

Efflux-pump inhibitors and therapeutic uses thereof Download PDF

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Publication number
CA2986083A1
CA2986083A1 CA2986083A CA2986083A CA2986083A1 CA 2986083 A1 CA2986083 A1 CA 2986083A1 CA 2986083 A CA2986083 A CA 2986083A CA 2986083 A CA2986083 A CA 2986083A CA 2986083 A1 CA2986083 A1 CA 2986083A1
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Canada
Prior art keywords
compound
methyl
formula
phenyl
asc
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CA2986083A
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English (en)
French (fr)
Inventor
Jurg Dreier
Berangere Gaucher
Eric Desarbre
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Basilea Pharmaceutica International AG
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Basilea Pharmaceutica International AG
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Publication of CA2986083A1 publication Critical patent/CA2986083A1/en
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4465—Non condensed piperidines, e.g. piperocaine only substituted in position 4
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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US11938114B2 (en) 2017-03-10 2024-03-26 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
WO2018165612A1 (en) 2017-03-10 2018-09-13 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
CN110770224B (zh) 2017-03-10 2022-11-18 罗格斯新泽西州立大学 作为外排泵抑制剂的吲哚衍生物
EP3630109A4 (en) 2017-05-26 2021-03-17 Rutgers, the State University of New Jersey BACTERIAL EFFLUX PUMP INHIBITORS
WO2019005841A1 (en) 2017-06-26 2019-01-03 Rutgers, The State University Of New Jersey THERAPEUTIC COMPOUNDS AND METHODS FOR TREATING INFECTION
CN111960970B (zh) * 2018-08-08 2021-08-20 中国人民解放军总医院 抗肿瘤化合物
CN114031786B (zh) * 2021-11-06 2022-12-09 大连理工大学 一种用于烷烃c-h键活化偶联反应的金属有机框架的制备方法及其应用

Family Cites Families (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4038412A (en) 1975-08-25 1977-07-26 Richardson-Merrell Inc. N-(phenylether-substituted benzyl)alkanediamines
DE2616484C3 (de) 1976-04-14 1981-02-26 A. Nattermann & Cie Gmbh, 5000 Koeln Basische Benzoyläther, deren Salze und quartäre Ammoniumverbindungen sowie Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
CA1118422A (en) 1978-11-20 1982-02-16 Herbert J. Havera Trans-2-substituted-amido-hexahydrobenzo [a] quinolizines
IL94466A (en) 1989-05-25 1995-01-24 Erba Carlo Spa Pharmaceutical preparations containing the history of A-amino carboxamide N-phenylalkyl are converted into such new compounds and their preparation
IE903196A1 (en) 1989-09-05 1991-03-13 Searle & Co Substituted n-benzylpiperidine amides
US5212182A (en) 1990-10-03 1993-05-18 American Home Products Corpooration Substituted quinolinyl- and naphthalenylbenzamides or benzylamines and related compounds useful as analgesics
GB9321812D0 (en) 1993-10-22 1993-12-15 Smithkline Beecham Plc Pharmaceuticals
US5432198A (en) 1994-08-18 1995-07-11 Sphinx Pharmaceuticals Corporation Vicinal-substituted carbocyclic compounds as therapeutic agents
US6506876B1 (en) 1994-10-11 2003-01-14 G.D. Searle & Co. LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use
US5585492A (en) 1994-10-11 1996-12-17 G. D. Searle & Co. LTA4 Hydrolase inhibitors
GB9515412D0 (en) 1995-07-27 1995-09-27 Pharmacia Spa 2-(4-substituted)-benzylamino-2-methyl-propanamide derivatives
AU4020897A (en) 1996-08-17 1998-03-06 Zeneca Limited 3-mercaptopyrrolidines as farnesyl protein transferase inhibitors
US6207665B1 (en) 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
UA52797C2 (uk) 1997-11-20 2003-01-15 Тейдзін Лімітед Похідне біфеніламідину, проліки, інгібітор коагуляції крові, агент для профілактики тромбозу або емболії та агент для терапії тромбозу або емболії
TR200001962T2 (tr) 1997-12-19 2001-01-22 Novo Nordisk A/S Fenol oksitleyen bir enzim yoluyla polisakkaridlerin modifikasyonu
US6399629B1 (en) 1998-06-01 2002-06-04 Microcide Pharmaceuticals, Inc. Efflux pump inhibitors
AU4614100A (en) 1999-05-17 2000-12-05 Teijin Limited Cyanobiphenyl derivatives
DE60023926T2 (de) * 1999-09-10 2006-07-20 Merck & Co., Inc. Tyrosin kinase inhibitoren
AU7961100A (en) 1999-10-28 2001-05-08 Daiichi Pharmaceutical Co., Ltd. Drug discharge pump inhibitors
WO2001049288A1 (en) 2000-01-06 2001-07-12 Merck Frosst Canada & Co. Novel compounds and compositions as protease inhibitors
AU2868601A (en) 2000-01-27 2001-08-07 Ribotargets Ltd Biaryl compounds, their preparation and their use in therapy
EP1686119B1 (en) * 2000-02-16 2009-07-29 Smithkline Beecham Plc Pyrimidine-5-one derivatives as LDL-PLA2 inhibitors
EP1339702A1 (en) 2000-03-15 2003-09-03 Warner-Lambert Company 5-amide substituted diarylamines as mek inhibitors
DE60115227T2 (de) 2000-05-11 2006-08-24 Bristol-Myers Squibb Co. Tetrahydroisochinolin-analoga als wachstumshormon-sekretagoga
US20020032238A1 (en) 2000-07-08 2002-03-14 Henning Priepke Biphenylcarboxylic acid amides, the preparation thereof and the use thereof as medicaments
HUP0500470A3 (en) 2000-09-01 2005-11-28 Fmc Corp 1,4-disubstituted benzenes as insecticides and use thereof
IL154363A0 (en) 2000-09-25 2003-09-17 Actelion Pharmaceuticals Ltd Substituted amino-aza-cycloalkanes useful against malaria
GB0024808D0 (en) 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
GB0024807D0 (en) 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
CN1489575A (zh) 2001-01-29 2004-04-14 ������������ʽ���� 苯甲脒衍生物及其制备方法
AR035425A1 (es) 2001-01-30 2004-05-26 Teijin Ltd Cristal de diclorhidrato del acido 3-(3-amidinofenil)-5-[({[1-(iminoetil)-4-piperidil]metil}amino)metil]benzoico y proceso para prepararlo
EP1372655B1 (en) 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
WO2002083641A2 (en) 2001-04-17 2002-10-24 Actelion Pharmaceuticals Ltd. Amino-aza-cyclohexanes for the treatment of malaria
US20030186963A1 (en) * 2001-09-14 2003-10-02 Dorwald Florencio Zaragoza Substituted piperidines
EP1430027B1 (en) 2001-09-14 2010-09-01 High Point Pharmaceuticals, LLC Novel aminoazetidine, -pyrrolidine and -piperidine derivatives
WO2003028720A1 (en) 2001-09-26 2003-04-10 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
AU2002363236A1 (en) 2001-10-30 2003-05-12 Millennium Pharmaceuticals, Inc. Compounds, pharmaceutical compositions and methods of use therefor
AU2002357692A1 (en) 2001-11-09 2003-05-26 Bristol-Myers Squibb Company Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
DE60335979D1 (de) 2002-02-13 2011-03-24 Ppg Ind Ohio Inc Rbundbeschichtung auf einem träger
US6660736B2 (en) 2002-03-27 2003-12-09 Hoffmann-La Roche Inc. Phthalimido derivatives and a process for their preparation
CA2482838A1 (en) 2002-05-31 2003-12-11 Eisai Co., Ltd. Pyrazole compounds and pharmaceutical compositions containing the compound
JP2005194193A (ja) 2002-06-11 2005-07-21 Taisho Pharmaceut Co Ltd ケモカイン受容体拮抗化合物
US20060063782A1 (en) 2002-07-03 2006-03-23 Murray Christopher W 3-Hetero arylmethoxy ! pyridines and their analogues as p38 map kinase inhibitors
EP1541558B1 (en) 2002-08-13 2008-08-13 Shionogi & Co., Ltd. Heterocyclic compounds having hiv integrase inhibitory activity
CA2851462A1 (en) 2003-01-08 2004-07-29 University Of Washington Antibacterial agents
CA2517256C (en) 2003-02-26 2013-04-30 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
WO2004081005A1 (en) * 2003-03-07 2004-09-23 Neurocrine Biosciences, Inc. Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
WO2004092123A2 (en) 2003-04-10 2004-10-28 Microbia, Inc. Inhibitors of fungal invasion
US7232825B2 (en) 2003-05-02 2007-06-19 Guoqing P Chen Phenylaminopyrimidine derivatives and methods of use
CA2530816A1 (en) * 2003-07-02 2005-01-13 Bayer Healthcare Ag Amide-substituted 1,2,4-triazin-5(2h)-ones for the treatment of chronic inflammatory diseases
WO2005002673A1 (en) 2003-07-03 2005-01-13 Astex Therapeutics Limited Raf kinase inhibitors
WO2005012270A2 (en) 2003-07-29 2005-02-10 Rib-X Pharmaceuticals, Inc. Biaryl heterocyclic amines, amides, and sulfur-containing compounds and methods of making and using the same
US7094791B2 (en) 2003-07-31 2006-08-22 Avalon Pharmaceuticals, Inc. Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof
US7572816B2 (en) 2003-08-01 2009-08-11 Auspex Pharmaceuticals, Inc. Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
JP2007513082A (ja) 2003-11-10 2007-05-24 シエーリング アクチエンゲゼルシャフト Ｃｃｒ−５アンタゴニストとして有用なベンジルエーテルアミン化合物
EP1535908A1 (en) 2003-11-24 2005-06-01 Newron Pharmaceuticals S.p.A. N-acyl-N'-benzyl-alkylendiamino drivatives
BRPI0418351A (pt) 2004-01-05 2007-05-08 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, métodos de limitar a proliferação celular em um humano ou animal, de tratamento de um humano ou animal sofrendo de cáncer, de tratamento de profilaxia de cáncer, de tratamento de um humano ou animal sofrendo de uma doença neoplásica, de tratamento de um humano ou animal sofrendo de uma doença prolifetativa de tratamento de cáncer, para o tratamento de infecções associadas com cáncer, para o tratamento profilático de infecções associadas com cáncer, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, método de inibir a chk1 quinase, e, processo para a preparação de um composto ou um sal farmaceuticamente aceitável do mesmo
US20090253908A1 (en) 2004-03-11 2009-10-08 Glaxo Group Limited Novel m3 muscarinic acetylchoine receptor antagonists
SE0401342D0 (sv) 2004-05-25 2004-05-25 Astrazeneca Ab Therapeutic compounds
WO2006028029A1 (ja) 2004-09-07 2006-03-16 Sankyo Company, Limited 置換ビフェニル誘導体
US7932247B2 (en) 2004-11-15 2011-04-26 Glaxo Group Limited M3 muscarinic acetylcholine receptor antagonists
ES2339138T3 (es) 2004-11-24 2010-05-17 Eli Lilly And Company Derivados de eteres aromaticos utiles como inhibidores de la trombina.
DE102004061008A1 (de) 2004-12-18 2006-06-22 Bayer Healthcare Ag 3-Arylalkyl- und 3-Heteroarylalkyl-substituierte 1,2,4-Triazin-5(2H)-one
DE102004061006A1 (de) 2004-12-18 2006-06-22 Bayer Healthcare Ag 3-Benzylthio-1,2,4-triazin-5(2H)-one
GT200600042A (es) 2005-02-10 2006-09-27 Aventis Pharma Inc Compuestos de bis arilo y heteroarilo sustituido como antagonistas selectivos de 5ht2a
NZ560969A (en) 2005-02-17 2010-08-27 Albany Molecular Res Inc Benzoxazole carboxamides for treating chemotherapy-induced vomiting and irritable bowel syndrome
US20070078172A1 (en) 2005-06-16 2007-04-05 Jenrin Discovery Mao-b inhibitors useful for treating obesity
US20070015832A1 (en) 2005-07-14 2007-01-18 Myriad Genetics, Incorporated Methods of treating overactive bladder and urinary incontinence
CA2625638C (en) 2005-11-08 2014-03-11 Surmodics, Inc. Ultra-thin photo-polymer coatings and uses thereof
WO2007079078A1 (en) * 2005-12-29 2007-07-12 Bayer Schering Pharma Aktiengesellschaft Diamine derivatives as inhibitors of leukotriene a4 hydrolase
ITMI20060179A1 (it) 2006-02-02 2007-08-03 Abiogen Pharma Spa Procedimento per la risoluzione di miscele racemiche e complesso diastereoisomerico di un agente risolvente e di unantiomero di interesse
CA2646076C (en) 2006-05-18 2015-06-30 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
TW200808705A (en) 2006-06-15 2008-02-16 Sanofi Aventis Aryl- and heteroaryl-ethyl-acylguanidine derivatives, their preparation and their application in therapeutics
US20110172230A1 (en) 2006-08-23 2011-07-14 Takahiro Ishii Urea compound or salt thereof
EP2102158A1 (en) 2006-12-11 2009-09-23 Topo Target A/S Prodrugs of diphenyl ox- indol- 2 -one compounds for the treatment of cancers
CL2007003874A1 (es) 2007-01-03 2008-05-16 Boehringer Ingelheim Int Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio
SA08280783B1 (ar) 2007-01-11 2011-04-24 استرازينيكا ايه بي مشتقات بيريدوبيريميدين كمثبطات pde4
CA2674865A1 (en) 2007-01-15 2008-07-24 Santen Pharmaceutical Co., Ltd. Indole derivative having i.kappa.b kinase .beta. inhibitory activity
US20080200454A1 (en) 2007-02-15 2008-08-21 Ameriks Michael K Carbon-linked tetrahydro-pyrazolo-pyridine modulators of cathepsin s
WO2008101195A2 (en) 2007-02-16 2008-08-21 Othera Holding, Inc. Drug resistance reversal in neoplastic disease
EP2620429A1 (en) 2007-02-22 2013-07-31 Colby Pharmaceutical Company Hydroxylamine compounds and methods of their use
JP2010120852A (ja) 2007-03-09 2010-06-03 Daiichi Sankyo Co Ltd 新規なジアミド誘導体
US20100256147A1 (en) * 2007-04-13 2010-10-07 Hangauer Jr David G Biaryl acetamide derivatives as modulators of the kinase cascade for the treatment of hearing loss, osteoporosis and cell proliferation disorders
EP3103791B1 (en) * 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
PE20090837A1 (es) 2007-07-02 2009-07-24 Boehringer Ingelheim Int Nuevos compuestos quimicos
AU2008311375A1 (en) 2007-10-10 2009-04-16 Merck Sharp & Dohme Corp. Diphenyl substituted cycloalkanes
US7932279B2 (en) 2007-10-12 2011-04-26 Arqule, Inc. Substituted tetrazole compounds and uses thereof
BRPI0821026A2 (pt) 2007-12-19 2015-06-16 Newron Pharmaceutical S P A Derivados de alfa-minoamidas úteis no tratamento de transtornos psiquiátricos
US20120009151A1 (en) * 2007-12-21 2012-01-12 Progenics Pharmaceuticals, Inc. Triazines And Related Compounds Having Antiviral Activity, Compositions And Methods Thereof
AR070563A1 (es) 2008-02-06 2010-04-21 Glaxo Group Ltd Compuesto de un biciclo condensado pirazol-piridin-amina, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento de enfermedades respiratorias.
PE20091553A1 (es) 2008-02-06 2009-10-30 Glaxo Group Ltd Farmacoforos duales - antagonistas muscarinicos de pde4
MY150379A (en) 2008-02-26 2013-12-31 Takeda Pharmaceutical Fused heterocyclic derivative and use thereof
WO2009130469A1 (en) 2008-04-25 2009-10-29 Kudos Pharmaceuticals Limited Dna-pk inhibitors
WO2009136625A1 (ja) * 2008-05-07 2009-11-12 大日本住友製薬株式会社 環状アミン－１－カルボン酸エステル誘導体およびそれを含有する医薬組成物
US20100035862A1 (en) 2008-06-25 2010-02-11 Abbott Laboratories Novel aza-cyclic indole-2-carboxamides and methods of use thereof
WO2010033643A2 (en) 2008-09-17 2010-03-25 Burnham Institute For Medical Research Small molecule compounds for stem cell differentiation
US9238657B2 (en) 2008-10-31 2016-01-19 Shionogi & Co., Ltd. Cephalosporin having catechol group
WO2010052448A2 (en) 2008-11-05 2010-05-14 Ucb Pharma S.A. Fused pyrazine derivatives as kinase inhibitors
WO2010111353A1 (en) 2009-03-25 2010-09-30 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
WO2010141817A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
PL2470173T3 (pl) 2009-08-25 2016-11-30 Leczenie skojarzone nanocząstkowymi kompozycjami taksanu i inhibitorów hedgehog
JP5781527B2 (ja) * 2009-10-30 2015-09-24 ヤンセン ファーマシューティカ エヌ．ベー． ４−置換−２−フェノキシ−フェニルアミンデルオピオイド受容体調節因子
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
TWI503323B (zh) 2010-03-29 2015-10-11 Oncotherapy Science Inc 三環化合物以及含此化合物之ｐｂｋ抑制劑
KR20130018845A (ko) 2010-04-05 2013-02-25 시오노기세야쿠 가부시키가이샤 카테콜기를 갖는 세펨 화합물
JP5823514B2 (ja) 2010-07-07 2015-11-25 アーデリクス，インコーポレーテッド リン酸輸送を阻害する化合物及び方法
WO2012006475A1 (en) 2010-07-07 2012-01-12 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
AR082498A1 (es) 2010-08-20 2012-12-12 Gruenenthal Gmbh Derivados ciclicos de carboxamida y urea sustituidos como ligandos del receptor de vainiloide
US8835472B2 (en) * 2010-09-02 2014-09-16 Boehringer Ingelheim International Gmbh Compounds, pharmaceutical compositions and uses thereof
US8722076B2 (en) 2010-09-30 2014-05-13 Surmodics, Inc. Photochrome- or near IR dye-coupled polymeric matrices for medical articles
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
WO2012079154A1 (en) 2010-12-14 2012-06-21 Dalhousie University Selective estrogen receptor modulators
CA2836202A1 (en) 2011-05-30 2012-12-06 Astellas Pharma Inc. Imidazopyridine compounds
JP2013047223A (ja) * 2011-07-28 2013-03-07 Otsuka Pharmaceut Co Ltd 医薬
GB201118876D0 (en) * 2011-11-01 2011-12-14 Astex Therapeutics Ltd Pharmaceutical compounds
TW201329025A (zh) * 2011-11-01 2013-07-16 Astex Therapeutics Ltd 醫藥化合物
CA2853833A1 (en) 2011-11-08 2013-05-16 Arena Pharmaceuticals, Inc. Modulators of the g protein-coupled mas receptor and the treatment of disorders related thereto
ES2668841T3 (es) 2011-11-29 2018-05-22 Vivozon Inc. Derivado novedoso de benzamida y uso del mismo
CN103130791B (zh) 2011-11-30 2016-05-04 正大天晴药业集团股份有限公司 一种新型苯甲酰胺类化合物
JP2013112657A (ja) 2011-11-30 2013-06-10 Toray Ind Inc フェノキシメチルベンズアミド誘導体、その薬学的に許容される酸付加塩及びその医薬用途
CN105030750B (zh) 2011-12-23 2018-08-28 中国医学科学院医药生物技术研究所 一组木豆素结构类似化合物在抗丙肝病毒和抗艾滋病毒的应用
RS54539B1 (sr) 2012-02-21 2016-06-30 Aziende Chimiche Riunite Angelini Francesco - A.C.R.A.F. - S.P.A. Upotreba 1h-indazol-3-karboksamidnih jedinjenja kao inhibitora kinaze 3-beta glikogen sintetaze
WO2013151991A1 (en) 2012-04-02 2013-10-10 Surmodics, Inc. Hydrophilic polymeric coatings for medical articles with visualization moiety
UY35103A (es) 2012-10-29 2014-05-30 Glaxo Group Ltd Compuestos de cefem 2-sustituidos
US9624214B2 (en) 2012-11-05 2017-04-18 Bayer Pharma Aktiengesellschaft Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
US9321764B2 (en) 2013-03-12 2016-04-26 Abbvie Inc. Dihydro-pyrrolopyridinone inhibitors
CA2913162C (en) 2013-05-22 2021-07-27 Curza Global, Llc Compositions and methods comprising a polyamine
US9914740B2 (en) 2013-07-02 2018-03-13 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
US9422285B2 (en) 2013-08-08 2016-08-23 Bayer Pharma Aktiengesellschaft Substituted pyrazolo[1,5-A]-pyridine-3-carboxamides and use thereof
JP6417419B2 (ja) 2013-09-04 2018-11-07 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 免疫調節剤として有用な化合物
EP2857388A1 (de) * 2013-10-01 2015-04-08 Grünenthal GmbH Sulfon-haltige Azole
US9458150B2 (en) * 2013-11-08 2016-10-04 Rutgers, The State University Of New Jersey Antimicrobial agents
HK1244211A1 (zh) 2014-11-14 2018-08-03 Melinta Therapeutics, Inc. 治疗、预防或降低皮肤感染风险的方法

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US10464896B2 (en) 2019-11-05
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KR20180011843A (ko) 2018-02-02
WO2016198691A1 (en) 2016-12-15
AU2016275764B8 (en) 2021-03-04
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US20200115339A1 (en) 2020-04-16
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US20180179158A1 (en) 2018-06-28
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