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AR054963A1 - Inhibidores de girasas y usos de los mismos - Google Patents

Inhibidores de girasas y usos de los mismos

Info

Publication number
AR054963A1
AR054963A1 ARP010105831A ARP010105831A AR054963A1 AR 054963 A1 AR054963 A1 AR 054963A1 AR P010105831 A ARP010105831 A AR P010105831A AR P010105831 A ARP010105831 A AR P010105831A AR 054963 A1 AR054963 A1 AR 054963A1
Authority
AR
Argentina
Prior art keywords
ylamino
benzimidazole
prop
ring
optionally substituted
Prior art date
Application number
ARP010105831A
Other languages
English (en)
Inventor
Anne-Laure Grillot
Paul Charifson
Dean Starnos
Yusheng Liao
Michael Badia
Martin Trudeau
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of AR054963A1 publication Critical patent/AR054963A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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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    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
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    • 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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    • C07D401/14—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 three or more hetero rings
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicacion 1: Un método para disminuir la cantidad de bacterias en una muestra biologica, método que comprende la etapa de poner en contacto dicha muestra biologica con un compuesto de formula (1), o una sal farmacéuticamente aceptable del mismo, en donde: Z es O o N- R4; W es nitrogeno o CRa ; Ra es seleccionado entre hidrogeno, halogeno,-CF3, R7, -OR7, o -N(R7)2, R1 es un anillo arilo o heteroarilo, en donde dicho anillo está sustituido opcionalmente por hasta cuatro R9; en donde un sustituyente R9 en la posicion orto de R1 tomado conjuntamente con R2 puede formar un anillo fusionado de 5-8 miembros no saturado o parcialmente no saturado, opcionalmente sustituido, que tiene 0-2 heteroátomos en el anillo seleccionados entre nitrogeno, oxígeno o azufre; R2 y R3 son cada uno seleccionado independientemente entre R6, halogeno, CN, SR6, OR6, N(R6)2, NRCO2R6, NRCON(R6)2, CON(R6)2, NRCOR6, NRN(R6)2, COR6, CO2R6, COCOR6, SO2R6, SO2N(R6)2 o NRSO2R6; o R2 y R3 son tomados conjuntamente para formar un anillo fusionado de 5-8 miembros opcionalmente sustituido, no saturado o parcialmente no saturado, que contiene de 0-2 heteroátomos en el anillo seleccionados entre nitrogeno, oxigeno, o azufre; R4 es seleccionado entre R6, CON(R6), COR6, CO2R6, COCOR6, SO2R6, SO2N(R6)2, o (CH2)yR2; y es 1-6; R5 es seleccionado entre R7, Ar, COAr, CON(R7)Ar, (CH2)yCO2R, (CH2)yN(R7)2, C(=NR10)-NRCOR, C(=S)-N(R7)2, CON(R7)2, CO2R, COR, SO2R, o SO2N(R7)2; Ar es un anillo de cinco miembros heteroarilo, heterociclilo, o carbociclilo, en donde dicho anillo está opcionalmente sustituido por hasta tres sustituyentes seleccionados entre oxo, halogeno, CN, NO2, R8, OR8, NHR8, NHCOR8, NHCONHR8, COR8, CONHR8, SO2R8, NHSO2NHR8 o SO2NHR8; cada R se selecciona independientemente de hidrogeno o un grupo alifático opcionalmente sustituido que tiene de uno a seis carbonos; cada R6 es seleccionado independientemente entre R7 o un grupo opcionalmente sustituido seleccionado entre alcoxi, hidroxialquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, aralcoxi, ariloxialquilo, heteroarilo, heteroaralquilo, heteroaralcoxi, o heteroariloxialquilo; cada R7 es seleccionado independientemente entre hidrogeno o un grupo alifático opcionalmente sustituido que tiene uno a seis carbonos, o dos R7 sobre el mismo nitrogeno tomados conjuntamente con el nitrogeno forman opcionalmente un anillo heterocíclico de cuatro a seis miembros, saturado o no saturado, que tiene uno a tres heteroátomos; R8 es un grupo alifático C1-4, en donde dos R8 sobre posiciones adyacentes de Ar, o un anillo arilo o heteroarilo, pueden ser tomados conjuntamente con los átomos a los cuales están unidos para formar un anillo fusionado de tres a seis miembros; cada R9 es seleccionado independientemente entre oxo, halogeno, CN, NO2, Tn(haloalquilo), R6, SR6, OR6, OR8, N(R6)2, CON(R6)2, CON( R )COR6, COR6, CO2R6, CO2N(R6)2, COCOR6, SO2R6, SO2N(R6)2, N(R) TnCO2R6, N(R)TnCON(R6)2, N(R)TnN(R6)2, N(R)TnNRCO2R6, N(R)TnNRCON(R6)2, N(R)TnCOR6, N(R)TnNRCOR6, N(R)TnSO2N(R6)2, N(R) TnSO2R6, TnPO(OR7)2, TnOPO(OR7)2, TnSP(OR7)2, TnPO(OR7)2 o TnNPO(OR7)2 cada Q es un alquilo C1-3, recto o ramificado, seleccionado independientemente; T es seleccionado entre -Q- o -Qm-CH(Qm-R2)-; cada m y n son seleccionados independientemente entre cero o uno; y R10 es seleccionado entre R7 o Ar con la condicion de que los siguientes compuestos queden excluidos: 2-[3-(3,5-dibromobencilamino)prop-1- ilamino]-1H-benzimidazol; 2-[3-(2-etoxi-3,5-dibromobencilamino)prop-1-ilamino]-1H-benzimidazol; 2-[3-(6,8-diclorocroman-4-ilamino)prop-1- ilamino]-1H-benzimidazol; 2-[3-(6,8-dibromo-1,2,3,4-tetrahidroquinolin-4-ilamino)prop-1-ilamino]1H-benzimidazol; 2-[3-(4,6-dicloroindol-2- ilmetilamino)prop-1-ilamino]-1H-benzimidazol; dihidrocloruro de 2(3-(6-etil-8-yodo-1,2,3,4-tetrahidroquinolin-4-ilamino)prop-1-ilamino]1H- benzimidazol; dihidrocloruro de 2-[3-(4,5-dibromotien-2-il)metilamino)prop-1-ilamino]- 1H-benzimidazol; 2-{3-[4,6-dicloro-1-(2-hidroxietil)-1H- indol-2-ilmetilamino]prop-1-ilamino} -1H-benzimidazol; 2-[3-(2-etoxi-3,5-diclorobenzilamino)prop-1-ilamino]-1H-benzimidazol; 2-[3-(3- bromo-2-etoxi-5-metoxibenciamino)prop-1-ilamino]-1H- benzimidazol; 2-[3-(2-etoxi-5-yodo-3-metilbencilamino)prop-1-ilamino]1H- benzimidazol; 2-[3-(4-trifluorometil-6-metoxindol-2-ilmetilamino)prop-1-ilamino]-1H-benzimidazol; 2-[3-(3,5-dibromobencilamino)prop-1- ilamino]-5-metoxi-1H-benzimidazol; dihidrocloruro de 2-amino-5-(4-metoxipiridin-2-il)benzoxazol; dihidrocloruro de 2-amino-5-(4- metoxipiridin-2-il)-1-metilbenzimidazol; dihidrocloruro de 2-amino-1-etil-5-(4-metoxipiridin-2-il)benzimidazol; dihidrocloruro de 2-amino-5-(4- metoxipiridin- 2-il)-1-fenilbenzimidazol; dihidrocloruro de 2-amino-5-(4-metoxipiridin-2-il)benzimidazol.
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Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2489128C (en) * 2002-06-13 2012-01-03 Vertex Pharmaceuticals Incorporated 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase iv inhibitors for the treatment of bacterial infections
AU2003266668A1 (en) * 2002-09-30 2004-04-23 Banyu Pharmaceutical Co., Ltd. 2-aminobenzimidazole derivative
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
US8404852B2 (en) 2003-01-31 2013-03-26 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7582641B2 (en) 2003-01-31 2009-09-01 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7569591B2 (en) * 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7618974B2 (en) 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US8193352B2 (en) 2003-01-31 2012-06-05 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
FR2852957B1 (fr) * 2003-03-31 2005-06-10 Sod Conseils Rech Applic Nouveaux derives d'imidazo-pyridine et leur utilisation en tant que medicament
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
US20050221357A1 (en) * 2003-09-19 2005-10-06 Mark Shannon Normalization of gene expression data
US20060024690A1 (en) * 2003-09-19 2006-02-02 Kao H P Normalization of data using controls
US20060029948A1 (en) * 2003-09-19 2006-02-09 Gary Lim Sealing cover and dye compatibility selection
US7417726B2 (en) * 2003-09-19 2008-08-26 Applied Biosystems Inc. Normalization of data using controls
US20050255485A1 (en) * 2004-05-14 2005-11-17 Livak Kenneth J Detection of gene duplications
WO2005121132A1 (ja) * 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗ｈｃｖ作用を有する縮合ヘテロ環化合物
JP2008515874A (ja) 2004-10-07 2008-05-15 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 抗菌薬
US20060233809A1 (en) * 2005-02-08 2006-10-19 Smith Gary J Method for treating prostate conditions
PE20070427A1 (es) * 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
EP1948635A1 (en) 2005-11-07 2008-07-30 Vertex Pharmaceuticals Incorporated Benzimidazole derivatives as gyrase inhibitors
EP2028936A4 (en) * 2006-02-13 2014-02-26 Univ Boston COMPOSITIONS AND METHODS FOR ANTIBIOTIC REINFORCEMENT AND ACTIVE INFLUENCE
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
GB0612428D0 (en) * 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents
US8481544B2 (en) 2006-06-22 2013-07-09 Biota Europe Limited Antibacterial compositions
AU2012200669B2 (en) * 2006-06-22 2012-11-01 Biota Europe Ltd Antibacterial compositions
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008019292A2 (en) * 2006-08-04 2008-02-14 Trustees Of Boston University Compositions and methods for potentiating antibiotic activity
AU2007330600B2 (en) * 2006-12-04 2012-05-10 Astrazeneca Ab Antibacterial polycyclic urea compounds
WO2009001915A1 (ja) * 2007-06-28 2008-12-31 Takeda Pharmaceutical Company Limited 置換イミダゾール化合物およびその用途
WO2009027732A1 (en) * 2007-08-24 2009-03-05 Astrazeneca Ab 5-6-bicyclic heteroaromatic compounds with antibacterial activity
AR069599A1 (es) * 2007-12-07 2010-02-03 Vertex Pharma Forma cristalina de 1- etil-1-3-(5-(5- fluoropiridin -3-il)-7- (pirimidin-2-il)-1h-benzo (d) imidazol -2-il) urea
GB0724342D0 (en) * 2007-12-13 2008-01-30 Prolysis Ltd Anitbacterial compositions
CL2009001345A1 (es) * 2008-06-04 2010-06-11 Astrazeneca Ab Compuestos derivados de 1-piridin-2-il-urea y 1-pirimidin-2-il-urea sustituidos, inhibidores de adn girasa y topoisomerasa iv; composicion farmaceutica; y su uso en tratamiento de infecciones bacterianas como neumonia adquirida intrahospitalariamente, infecciones a la piel, bronquitis, sinusitis, entre otras enfermedades.
KR20110031419A (ko) * 2008-06-04 2011-03-28 아스트라제네카 아베 항박테리아제로서의 티아졸로［５,４­ｂ］피리딘 및 옥사졸로［５,４­ｂ］피리딘 유도체
TW201000475A (en) 2008-06-04 2010-01-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
GB0821913D0 (en) 2008-12-02 2009-01-07 Price & Co Antibacterial compounds
TW201026695A (en) 2008-12-12 2010-07-16 Astrazeneca Ab Piperidine compounds and uses thereof-596
TW201026694A (en) 2008-12-12 2010-07-16 Astrazeneca Ab Compound 468
TW201102065A (en) 2009-05-29 2011-01-16 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
MX2011012961A (es) 2009-06-05 2012-01-30 Cephalon Inc Preparacion y usos de derivados de 1,2,4-triazolo[1,5a]-piridina.
TR201900259T4 (tr) 2009-08-17 2019-02-21 Intellikine Llc Heterosiklik Bileşikler Ve Bunların Kullanımları
UY32856A (es) 2009-08-26 2011-03-31 Astrazeneca Ab Derivados heterocíclicos de urea y métodos de uso de los mismos
EP2475666A2 (en) 2009-09-11 2012-07-18 Trius Therapeutics, Inc. Gyrase inhibitors
US20130096119A1 (en) 2010-03-31 2013-04-18 Daniel Bur Isoquinolin-3-Ylurea Derivatives
JP5894980B2 (ja) 2010-05-24 2016-03-30 インテリカイン， エルエルシー 複素環式化合物およびその使用
WO2011151618A2 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile-associated disease
WO2011151619A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
WO2011151620A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
RS54781B1 (sr) 2010-06-01 2016-10-31 Summit Therapeutics Plc Jedinjenja za lečenje bolesti povezane sa clostridium difficile
WO2011151617A1 (en) 2010-06-01 2011-12-08 Summit Corporation Plc Compounds for the treatment of clostridium difficile associated disease
AU2011313820A1 (en) * 2010-10-08 2013-04-11 Biota Europe Ltd Antibacterial compounds
CN103443096B (zh) * 2011-01-14 2016-06-29 沃泰克斯药物股份有限公司 促旋酶和拓扑异构酶iv抑制剂
US8476281B2 (en) 2011-01-14 2013-07-02 Vertex Pharmaceuticals Incorporated Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea
AU2012205420B2 (en) 2011-01-14 2016-12-08 Spero Therapeutics, Inc. Process of making gyrase and topoisomerase IV inhibitors
SG191924A1 (en) * 2011-01-14 2013-08-30 Vertex Pharma Solid forms of gyrase inhibitor (r)-1-ethyl-3-[5-[2-{1-hydroxy-1-methyl-ethyl}pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urea
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
AR085397A1 (es) 2011-02-23 2013-09-25 Intellikine Inc Combinacion de inhibidores de quinasa y sus usos
AR088729A1 (es) 2011-03-29 2014-07-02 Actelion Pharmaceuticals Ltd Derivados de 3-ureidoisoquinolin-8-ilo y una composicion farmaceutica
ES2576298T3 (es) 2011-06-20 2016-07-06 Vertex Pharmaceuticals Incorporated Ésteres de fosfato de inhibidores de girasa y topoisomerasa
WO2013016720A2 (en) * 2011-07-28 2013-01-31 Gerinda Therapeutics, Inc. Novel substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
KR101546743B1 (ko) 2012-01-16 2015-08-24 한국과학기술원 인돌 유도체 화합물, 이를 포함하는 Ａｂｌ 키나제 저해제 조성물 및 이상세포 성장 질환의 예방 및 치료용 약학 조성물
US9572809B2 (en) 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
TWI595002B (zh) 2012-07-18 2017-08-11 思沛羅三南公司 （Ｒ）－２－（５－（２－（３－乙基脲基）－６－氟－７－（四氫呋喃－２－基）－１Ｈ－苯并［ｄ］咪唑－５－基）嘧啶－２－基）丙烷－２－基磷酸二氫鹽之固體形式及其鹽
US9079935B2 (en) 2012-08-13 2015-07-14 The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Reducing risk of contracting Clostridium-difficile associated disease
JP2015526520A (ja) 2012-08-31 2015-09-10 プリンシピア バイオファーマ インコーポレイテッド Ｉｔｋ阻害剤としてのベンズイミダゾール誘導体
US9988373B2 (en) 2013-12-26 2018-06-05 Shionogi & Co., Ltd. Nitrogen-containing six-membered cyclic derivatives and pharmaceutical composition comprising the same
US20170007615A1 (en) 2014-02-03 2017-01-12 Biota Europe Ltd Antibacterial Compounds
CN104876878B (zh) * 2014-02-27 2018-04-27 中国科学院广州生物医药与健康研究院 5-芳基酚-2烷基取代脲苯并咪唑类化合物及其应用
WO2016127102A2 (en) 2015-02-06 2016-08-11 Ernesto Abel-Santos Inhibiting germination of clostridium perfringens spores to reduce necrotic enteritis
CN107641118B (zh) * 2016-07-22 2020-11-06 爱科诺生物医药股份有限公司 具有细胞坏死抑制活性的化合物及其组合物和应用
US11180459B2 (en) * 2017-03-10 2021-11-23 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
US20210070747A1 (en) 2017-03-24 2021-03-11 Taisho Pharmaceutical Co., Ltd. 2(1h)-quinolinone derivative
WO2018213185A1 (en) 2017-05-17 2018-11-22 Drexel University Rela inhibitors for biofilm disruption
US20200237717A1 (en) * 2017-08-01 2020-07-30 Opal Biosciences Limited Treatment of Staphylococcal and Enterococcal Infections Using Substituted Nitrostyrene Compounds
RU2643372C1 (ru) * 2017-08-07 2018-02-01 Федеральное государственное бюджетное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" Способ получения этил 3-(3-гидрокси-1,4-диоксо-1,4-дигидронафталин-2-ил)-2,5,10-триоксо-10b-фенил-1,2,3,5,10,10b-гексагидро-3аН-нафто[2',3':4,5]фуро[3,2-b]пиррол-3а-карбоксилатов
CN113194752A (zh) 2018-06-01 2021-07-30 康奈尔大学 Pi3k相关疾病或病症的组合疗法
US12258342B2 (en) 2018-09-03 2025-03-25 Univerza V Ljubljani Class of DNA gyrase and/or topoisomerase IV inhibitors with activity against gram-positive and gram-negative bacteria
CA3146788C (en) 2019-07-17 2024-06-18 Summit (Oxford) Limited Process for the preparation of ridinilazole and crystalline forms thereof
CN110622973B (zh) * 2019-11-06 2020-11-10 海南大学 1-芳基-4-吡啶酮类化合物的应用
US20250002455A1 (en) 2020-12-17 2025-01-02 Univerza V Ljubljani New n-phenylpyrrolamide inhibitors of dna gyrase and topoisomerase iv with antibacterial activity
GB202100471D0 (en) 2021-01-14 2021-03-03 Summit Oxford Ltd Preparation of antibacterial compounds
GB202100470D0 (en) 2021-01-14 2021-03-03 Summit Oxford Ltd Solid tablet dosage for of ridinilazole
US12220421B2 (en) 2021-09-09 2025-02-11 The Boards Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Inhibitors of C. difficile spore germination
WO2024249488A2 (en) * 2023-05-30 2024-12-05 Beth Israel Deaconess Medical Center, Inc. Inhibitors of dyrk1a

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4174400A (en) * 1978-09-13 1979-11-13 Merck & Co., Inc. Anthelmintic benzimidazoles
US4338315A (en) * 1979-11-14 1982-07-06 Eli Lilly And Company Antiviral method employing thiazinyl benzimidazole derivatives
US4512998A (en) 1980-10-20 1985-04-23 Schering Corporation Anthelmintic benzimidazole carbamates
US4401817A (en) * 1981-04-20 1983-08-30 Eli Lilly And Company Carbonyl-substituted 1-sulfonylbenzimidazoles
GB8803429D0 (en) * 1988-02-15 1988-03-16 Fujisawa Pharmaceutical Co Imidazole compounds processes for preparation thereof & pharmaceutical composition comprising same
FR2643903A1 (fr) * 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US5296486A (en) * 1991-09-24 1994-03-22 Boehringer Ingelheim Pharmaceuticals, Inc. Leukotriene biosynthesis inhibitors
DE4317657C1 (de) * 1993-05-27 1994-07-14 Voith Gmbh J M Streicheinrichtung zur Beschichtung laufender Warenbahnen
PT759774E (pt) 1993-09-22 2002-11-29 Xoma Technology Ltd Metodo para o tratamento de infeccoes bacterianas gram-negativas por administracao de um produto de proteina bactericida indutora da permeabilidade (bip) e de um antibiotico
ES2179095T3 (es) 1994-01-14 2003-01-16 Xoma Technology Ltd Metodos y materiales anti bacterias gram positivas.
DE19514313A1 (de) * 1994-08-03 1996-02-08 Bayer Ag Benzoxazolyl- und Benzothiazolyloxazolidinone
HRP960159A2 (en) * 1995-04-21 1997-08-31 Bayer Ag Benzocyclopentane oxazolidinones containing heteroatoms
TW538046B (en) * 1998-01-08 2003-06-21 Hoechst Marion Roussel Inc Aromatic amides having antiobiotic activities and the preparation processes, intermediates and pharmaceutical composition thereof
AUPP873799A0 (en) * 1999-02-17 1999-03-11 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds
GB9911594D0 (en) * 1999-05-19 1999-07-21 Smithkline Beecham Plc Novel compounds
GB9912413D0 (en) * 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy

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JP2009102449A (ja) 2009-05-14
US20040043989A1 (en) 2004-03-04
AU2006201397A1 (en) 2006-04-27
US7414046B2 (en) 2008-08-19
PL362691A1 (en) 2004-11-02
BR0116216A (pt) 2004-08-17
ATE375983T1 (de) 2007-11-15
ES2331250T3 (es) 2009-12-28
US20030119868A1 (en) 2003-06-26
MY138797A (en) 2009-07-31
NO20032668D0 (no) 2003-06-12
ES2294046T3 (es) 2008-04-01
KR100944645B1 (ko) 2010-03-04
DE60131015D1 (de) 2007-11-29
CN1481368A (zh) 2004-03-10
US6632809B2 (en) 2003-10-14
IL156031A (en) 2011-11-30
PT1341769E (pt) 2007-12-31
WO2002060879A3 (en) 2003-03-27
NZ526241A (en) 2007-01-26
ATE443052T1 (de) 2009-10-15
DE60139964D1 (de) 2009-10-29
MXPA03005298A (es) 2003-10-06
AP2003002824A0 (en) 2003-09-30
CA2433197C (en) 2009-11-24
HUP0303494A2 (hu) 2004-01-28
RU2262932C2 (ru) 2005-10-27
KR20030061855A (ko) 2003-07-22
EP1341769A2 (en) 2003-09-10
WO2002060879A2 (en) 2002-08-08
SI1341769T1 (sl) 2008-02-29
HK1061851A1 (en) 2004-10-08
EP1341769B1 (en) 2007-10-17

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