AU2012229997B2 - Tricyclic gyrase inhibitors - Google Patents

Tricyclic gyrase inhibitors Download PDF

Info

Publication number
AU2012229997B2
AU2012229997B2 AU2012229997A AU2012229997A AU2012229997B2 AU 2012229997 B2 AU2012229997 B2 AU 2012229997B2 AU 2012229997 A AU2012229997 A AU 2012229997A AU 2012229997 A AU2012229997 A AU 2012229997A AU 2012229997 B2 AU2012229997 B2 AU 2012229997B2
Authority
AU
Australia
Prior art keywords
compound
nhme
mmol
pct
hnn
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
AU2012229997A
Other languages
English (en)
Other versions
AU2012229997A1 (en
Inventor
Paul ARISTOFF
Daniel Bensen
Zhiyong Chen
John Finn
Michael Jung
Thanh To Lam
Suk Joong Lee
Xiaoming Li
Felice LIGHTSTONE
Toan B. Nguyen
Douglas W. Phillipson
Leslie William Tari
Michael Trzoss
Sergio E. Wong
Junhu Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Lawrence Livermore National Security LLC
Original Assignee
Merck Sharp and Dohme LLC
Lawrence Livermore National Security LLC
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 Merck Sharp and Dohme LLC, Lawrence Livermore National Security LLC filed Critical Merck Sharp and Dohme LLC
Publication of AU2012229997A1 publication Critical patent/AU2012229997A1/en
Assigned to LAWRENCE LIVERMORE NATIONAL SECURITY, LLC, MERCK SHARP & DOHME CORP. reassignment LAWRENCE LIVERMORE NATIONAL SECURITY, LLC Request for Assignment Assignors: LAWRENCE LIVERMORE NATIONAL SECURITY, LLC, TRIUS THERAPEUTICS INC.
Application granted granted Critical
Publication of AU2012229997B2 publication Critical patent/AU2012229997B2/en
Assigned to LAWRENCE LIVERMORE NATIONAL SECURITY, LLC, MERCK SHARP & DOHME LLC reassignment LAWRENCE LIVERMORE NATIONAL SECURITY, LLC Request for Assignment Assignors: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2012229997A 2011-03-15 2012-03-14 Tricyclic gyrase inhibitors Active AU2012229997B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161453011P 2011-03-15 2011-03-15
US61/453,011 2011-03-15
PCT/US2012/029104 WO2012125746A1 (en) 2011-03-15 2012-03-14 Tricyclic gyrase inhibitors

Publications (2)

Publication Number Publication Date
AU2012229997A1 AU2012229997A1 (en) 2013-09-19
AU2012229997B2 true AU2012229997B2 (en) 2016-04-14

Family

ID=45879060

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012229997A Active AU2012229997B2 (en) 2011-03-15 2012-03-14 Tricyclic gyrase inhibitors

Country Status (16)

Country Link
US (2) US9732083B2 (https=)
EP (1) EP2686320B1 (https=)
JP (1) JP6140083B2 (https=)
KR (2) KR20140059164A (https=)
CN (1) CN103562208B (https=)
AR (1) AR085806A1 (https=)
AU (1) AU2012229997B2 (https=)
BR (1) BR112013023266B8 (https=)
CA (1) CA2829939C (https=)
IL (1) IL228220A (https=)
MX (1) MX345780B (https=)
PH (1) PH12013501800A1 (https=)
RU (1) RU2626979C2 (https=)
TW (1) TWI527818B (https=)
WO (1) WO2012125746A1 (https=)
ZA (1) ZA201307583B (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2686320B1 (en) * 2011-03-15 2016-05-18 Merck Sharp & Dohme Corp. Tricyclic gyrase inhibitors
EP2807165B1 (en) * 2012-01-27 2019-05-15 Université de Montréal Pyrimido[4,5-b]indole derivatives and use thereof in the expansion of hematopoietic stem cells
CN105189505B (zh) * 2012-09-12 2019-03-22 默克夏普&多梅有限公司 用作抗菌剂的三环促旋酶抑制剂
CN103304488B (zh) * 2013-06-13 2015-12-09 暨明医药科技（苏州）有限公司 光学纯2-（1-羟基乙基）-5-羟基嘧啶的制备方法
CN105899511B (zh) * 2013-09-11 2019-06-07 默沙东公司 三环促旋酶抑制剂
US20170007615A1 (en) 2014-02-03 2017-01-12 Biota Europe Ltd Antibacterial Compounds
WO2015150337A1 (en) * 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
CA3057431A1 (en) 2017-03-24 2018-09-27 Taisho Pharmaceutical Co., Ltd. 2(1h)-quinolinone derivative
CN110475777B (zh) * 2017-03-30 2022-04-15 豪夫迈·罗氏有限公司 用于治疗和预防细菌感染的新吡啶并[2,3-b]吲哚化合物
CN108504647B (zh) * 2018-03-09 2021-11-05 中山大学 一种dna促旋酶的药物结合口袋及其应用
JP7296992B2 (ja) * 2018-05-28 2023-06-23 エフ． ホフマン－ラ ロシュ アーゲー 細菌感染症の処置および予防のための新規オキソキノリジン化合物
WO2020064661A1 (en) * 2018-09-26 2020-04-02 F. Hoffmann-La Roche Ag Substituted pyridoindoles for the treatment and prophylaxis of bacterial infection
EP3887370B1 (en) * 2018-11-27 2023-01-18 F. Hoffmann-La Roche AG Tricyclic compounds for the treatment and prophylaxis of bacterial infection
WO2020109191A1 (en) 2018-11-27 2020-06-04 F. Hoffmann-La Roche Ag Aryl compounds for the treatment and prophylaxis of bacterial infection
WO2020127624A1 (en) 2018-12-20 2020-06-25 F. Hoffmann-La Roche Ag Oxopyrido[1,2-a]pyrimidine compounds for the treatment and prophylaxis of bacterial infection
CN114763357B (zh) * 2021-01-15 2024-06-18 中国科学院上海药物研究所 吲哚并嘧啶三环类化合物及其制备方法和用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050227992A1 (en) * 2003-10-14 2005-10-13 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein kinase inhibitors

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN157280B (https=) 1983-07-15 1986-02-22 Hoechst India
CA1336090C (en) 1988-08-31 1995-06-27 Isao Hayakawa Spiro-substituted cyclic amines of quinolone derivatives
DE4030059A1 (de) 1990-09-22 1992-03-26 Bayer Ag Verfahren zur herstellung von 5-hydroxy-3,4,5,6-tetrahydro-pyrimidin-derivaten
DE4032560A1 (de) 1990-10-13 1992-04-16 Bayer Ag 7-(2,7-diazabicyclo(3.3.0)octyl)-3-chinolon- und -naphtyridoncarbonsaeure-derivate
ES2150941T3 (es) 1992-04-03 2000-12-16 Upjohn Co Aminas biciclicas-heterociclicas eficaces farmaceuticamente.
US5279359A (en) 1992-06-26 1994-01-18 Erickson Donald C Rotary trisorption heat pump
US5350791A (en) 1992-07-02 1994-09-27 Henkel Corporation Hydrophilicizing treatment for metal objects
US5527910A (en) 1992-12-30 1996-06-18 Cheil Foods & Chemicals, Inc. Pyridone carboxylic acid compounds and their uses for treating infectious diseases caused by bacteria
RU2158127C2 (ru) * 1994-12-23 2000-10-27 Варнер-Ламберт Компани Способы ингибирования тирозинкиназы рецептора эпидермального фактора роста, азотсодержащие трициклические соединения, фармацевтическая композиция, предназначенная для введения ингибитора тирозинкиназы рецептора эпидермального фактора роста, например, erb-b2, erb-b3 или erb-b4, и противозачаточная композиция
NZ304519A (en) 1995-03-02 2000-01-28 Upjohn Co Pydrimido[4,5-b]indoles
SI9620103A (sl) * 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
WO1998029397A1 (en) 1996-12-27 1998-07-09 Yoshitomi Pharmaceutical Industries, Ltd. Fused pyrimidine compounds and medicinal use thereof
SI0964865T1 (en) 1997-01-08 2003-08-31 Pharmacia & Upjohn Company Pharmaceutically active tricyclic amines
ATE265847T1 (de) 1997-07-29 2004-05-15 Upjohn Co Selbstemulgierbare formulierung enthaltend lipophile verbindungen
US6147085A (en) 1999-04-01 2000-11-14 Neurogen Corporation Aminoalkyl substituted 9H-pyridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives
EP1068207A1 (en) 1998-04-02 2001-01-17 Neurogen Corporation AMINOALKYL SUBSTITUTED 9H-PYRIDINO 2,3-b]INDOLE AND 9H-PYRIMIDINO 4,5-b]INDOLE DERIVATIVES
US6221875B1 (en) 1998-04-02 2001-04-24 Neurogen Corporation Substituted 9H-pyridino [2,3-B]indole and 9H-pyrimidino [4,5-B]indole derivatives: selective neuropeptide Y receptor ligands
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
WO2000066585A1 (en) 1999-04-30 2000-11-09 Neurogen Corporation 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS
SK10572002A3 (sk) 2000-01-24 2003-10-07 Warner-Lambert Company 3-Aminochinazolín-2,4-diónové antibakteriálne činidlá
FR2816509B1 (fr) 2000-11-15 2004-02-06 Sod Conseils Rech Applic Association d'inhibiteurs de calpaine et de piegeurs des formes reactives de l'oxygene
JP2005515173A (ja) 2001-10-31 2005-05-26 バイエル・ヘルスケア・アクチェンゲゼルシャフト ピリミド［４，５−ｂ］インドール誘導体
CA2466266A1 (en) * 2001-11-08 2003-07-31 Antex Pharma, Inc. Novel substituted alkane compounds and uses thereof
WO2003057149A2 (en) 2001-12-28 2003-07-17 Bayer Corporation 4-substituted fused heteropyrimidines and fused hetero-4-pyrimidones
TWI270549B (en) 2002-12-26 2007-01-11 Taisho Pharmaceutical Co Ltd Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with cyclic amino group
WO2004058764A1 (en) * 2002-12-27 2004-07-15 Bayer Healthcare Ag 4-phenyl-pyrimido [4,5-b] indole derivatives
US20090143399A1 (en) 2003-10-14 2009-06-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
US20080051414A1 (en) 2003-10-14 2008-02-28 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
US20090099165A1 (en) 2003-10-14 2009-04-16 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
JP2006036762A (ja) 2004-06-25 2006-02-09 Taisho Pharmaceut Co Ltd 環状アミノ基で置換されているピロロピリミジン及びピロロピリジン誘導体
JP2007161585A (ja) 2004-06-25 2007-06-28 Taisho Pharmaceut Co Ltd 環状アミノ基で置換されているピロロピリミジン及びピロロピリジン誘導体
WO2008007113A2 (en) 2006-07-14 2008-01-17 Astex Therapeutics Limited Pharmaceutical combinations
CA2604284A1 (en) 2005-04-28 2006-11-02 Supergen, Inc. Protein kinase inhibitors
EP1749822B1 (en) * 2005-08-05 2008-10-15 Hybrigenics S.A. Novel cysteine protease inhibitors and their therapeutic applications
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
JP2007169216A (ja) 2005-12-22 2007-07-05 Taisho Pharmaceut Co Ltd 環状アミノ基で置換されているピロロピリミジン及びピロロピリジン誘導体
US20080207632A1 (en) 2006-10-31 2008-08-28 Supergen, Inc. Protein kinase inhibitors
US8618121B2 (en) 2007-07-02 2013-12-31 Cancer Research Technology Limited 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors
US7982035B2 (en) 2007-08-27 2011-07-19 Duquesne University Of The Holy Spirit Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
US7960400B2 (en) * 2007-08-27 2011-06-14 Duquesne University Of The Holy Ghost Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
WO2009091476A1 (en) 2008-01-14 2009-07-23 Irm Llc Compositions and methods for treating cancers
ATE546448T1 (de) * 2008-08-02 2012-03-15 Janssen Pharmaceutica Nv Urotensin-ii-rezeptorantagonisten
WO2011056739A1 (en) 2009-11-03 2011-05-12 Glaxosmithkline Llc Compounds and methods
EP2686320B1 (en) * 2011-03-15 2016-05-18 Merck Sharp & Dohme Corp. Tricyclic gyrase inhibitors
CN105189505B (zh) * 2012-09-12 2019-03-22 默克夏普&多梅有限公司 用作抗菌剂的三环促旋酶抑制剂
CN105899511B (zh) * 2013-09-11 2019-06-07 默沙东公司 三环促旋酶抑制剂
WO2016067009A1 (en) * 2014-10-28 2016-05-06 Redx Pharma Plc Compounds with activity against bacteria and mycobacteria

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050227992A1 (en) * 2003-10-14 2005-10-13 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein kinase inhibitors

Also Published As

Publication number Publication date
WO2012125746A1 (en) 2012-09-20
IL228220A0 (en) 2013-11-25
BR112013023266A8 (pt) 2018-06-12
MX2013010511A (es) 2014-03-27
RU2013140798A (ru) 2015-04-20
IL228220A (en) 2017-04-30
CN103562208B (zh) 2016-08-31
CN103562208A (zh) 2014-02-05
AU2012229997A1 (en) 2013-09-19
EP2686320A1 (en) 2014-01-22
MX345780B (es) 2017-02-15
KR102132574B1 (ko) 2020-07-09
EP2686320B1 (en) 2016-05-18
BR112013023266B8 (pt) 2021-04-06
CA2829939C (en) 2020-10-13
NZ614983A (en) 2016-07-29
US10858360B2 (en) 2020-12-08
PH12013501800A1 (en) 2013-10-14
KR20140059164A (ko) 2014-05-15
TWI527818B (zh) 2016-04-01
ZA201307583B (en) 2014-08-27
JP2014508173A (ja) 2014-04-03
BR112013023266B1 (pt) 2020-12-29
RU2626979C2 (ru) 2017-08-02
US20120238751A1 (en) 2012-09-20
AR085806A1 (es) 2013-10-30
WO2012125746A9 (en) 2013-10-24
BR112013023266A2 (https=) 2017-09-12
TW201245200A (en) 2012-11-16
JP6140083B2 (ja) 2017-05-31
CA2829939A1 (en) 2012-09-20
KR20190104632A (ko) 2019-09-10
US20170369498A1 (en) 2017-12-28
US9732083B2 (en) 2017-08-15

Similar Documents

Publication Publication Date Title
AU2012229997B2 (en) Tricyclic gyrase inhibitors
US10865216B2 (en) Tricyclic Gyrase inhibitors
AU2008254588B2 (en) Heterocyclic kinase modulators
US8362018B2 (en) Substituted imidazo[1,2-a]pyrazine compounds useful for the treatment of viral infections
CA3137458A1 (en) Fgfr inhibitors and methods of use thereof
AU2021296607B2 (en) Capsid inhibitors for the treatment of HIV
CA3147902A1 (en) Heterobicyclic amides as inhibitors of cd38
WO2019165073A1 (en) Shp2 phosphatase inhibitors and methods of use thereof
US20190040084A1 (en) Heterocyclic compounds as rsv inhibitors
IL212499A (en) Pyrolopyrazinyl urea kinase inhibitors
BR112012000413A2 (pt) compostos e composições para o tratamento de doenças parasitárias
WO2013185202A1 (en) Apoptosis inducers
NZ614983B2 (en) Tricyclic gyrase inhibitors
JP2025520019A (ja) Ｖｈｌリガンドとしてのベンゾチアゾール化合物

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: LAWRENCE LIVERMORE NATIONAL SECURITY, LLC; MERCK S

Free format text: FORMER APPLICANT(S): TRIUS THERAPEUTICS INC.; LAWRENCE LIVERMORE NATIONAL SECURITY, LLC

FGA Letters patent sealed or granted (standard patent)
PC Assignment registered

Owner name: MERCK SHARP & DOHME LLC

Free format text: FORMER OWNER(S): LAWRENCE LIVERMORE NATIONAL SECURITY, LLC; MERCK SHARP & DOHME CORP.

Owner name: LAWRENCE LIVERMORE NATIONAL SECURITY, LLC

Free format text: FORMER OWNER(S): LAWRENCE LIVERMORE NATIONAL SECURITY, LLC; MERCK SHARP & DOHME CORP.