MX339455B - Inhibidores de pirimidina y topoisomerasa iv. - Google Patents

Inhibidores de pirimidina y topoisomerasa iv.

Info

Publication number
MX339455B
MX339455B MX2013008162A MX2013008162A MX339455B MX 339455 B MX339455 B MX 339455B MX 2013008162 A MX2013008162 A MX 2013008162A MX 2013008162 A MX2013008162 A MX 2013008162A MX 339455 B MX339455 B MX 339455B
Authority
MX
Mexico
Prior art keywords
gyrase
topoisomerase
inhibitors
compounds
formula
Prior art date
Application number
MX2013008162A
Other languages
English (en)
Other versions
MX2013008162A (es
Inventor
Anne-Laure Grillot
Emanuele Perola
Paul S Charifson
Arnaud Le Tiran
Youssef Laafiret Bennani
Hardwin O'dowd
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 MX2013008162A publication Critical patent/MX2013008162A/es
Publication of MX339455B publication Critical patent/MX339455B/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a un compuesto de la fórmula (I) o una sal farmacéuticamente aceptable del mismo en donde X y R son como se definen en este documento. Los compuestos de la fórmula (I) son útiles como inhibidores de girasa y/o topoisomerasa IV para tratar infecciones bacterianas. Los compuestos de la fórmula (I) poseen ya sea un amplio intervalo de actividad anti-bacteriana y propiedades toxicológicas ventajosas o son profármacos de compuestos que tienen la actividad.
MX2013008162A 2011-01-14 2012-01-13 Inhibidores de pirimidina y topoisomerasa iv. MX339455B (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161432965P 2011-01-14 2011-01-14
US201161499134P 2011-06-20 2011-06-20
US201161515249P 2011-08-04 2011-08-04
US201161515174P 2011-08-04 2011-08-04
PCT/US2012/021270 WO2012097269A1 (en) 2011-01-14 2012-01-13 Pyrimidine gyrase and topoisomerase iv inhibitors

Publications (2)

Publication Number Publication Date
MX2013008162A MX2013008162A (es) 2013-08-27
MX339455B true MX339455B (es) 2016-05-27

Family

ID=45567120

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013008162A MX339455B (es) 2011-01-14 2012-01-13 Inhibidores de pirimidina y topoisomerasa iv.

Country Status (18)

Country Link
US (2) US8481551B2 (es)
EP (1) EP2663557B1 (es)
JP (1) JP6085829B2 (es)
KR (1) KR101897952B1 (es)
CN (1) CN103443096B (es)
AR (1) AR084863A1 (es)
AU (1) AU2012205415B2 (es)
BR (1) BR112013017974B1 (es)
CA (1) CA2824516C (es)
CL (1) CL2013002025A1 (es)
ES (1) ES2545516T3 (es)
IL (1) IL227406A (es)
MX (1) MX339455B (es)
RU (1) RU2609259C2 (es)
SG (1) SG191946A1 (es)
TW (1) TWI546298B (es)
WO (1) WO2012097269A1 (es)
ZA (1) ZA201305233B (es)

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MX341342B (es) * 2011-01-14 2016-08-17 Vertex Pharma Formas solidas del inhibidor de girasa (r)-1-etil-3-[6-fluoro-5-[2 -(1-hidroxi-1-metil-etil) pirimidin-5-il]-7-(tetrahidrofuran-2-il) -1h-benzimidazol-2-il]urea.
SG191946A1 (en) 2011-01-14 2013-08-30 Vertex Pharma Pyrimidine gyrase and topoisomerase iv inhibitors
CN103384666A (zh) * 2011-01-14 2013-11-06 沃泰克斯药物股份有限公司 固体形式的促旋酶抑制剂(r)-1-乙基-3-[5-[2-(1-羟基-1-甲基-乙基)嘧啶-5-基]-7-(四氢呋喃-2-基)-1氢-苯并咪唑-2-基]脲
JP5977344B2 (ja) 2011-06-20 2016-08-24 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated ジャイレースおよびトポイソメラーゼ阻害剤のリン酸エステル
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WO2024112738A1 (en) * 2022-11-22 2024-05-30 University Of Maryland, Baltimore Bovine colostrum-derived nutritional supplements and uses thereof

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MX341342B (es) * 2011-01-14 2016-08-17 Vertex Pharma Formas solidas del inhibidor de girasa (r)-1-etil-3-[6-fluoro-5-[2 -(1-hidroxi-1-metil-etil) pirimidin-5-il]-7-(tetrahidrofuran-2-il) -1h-benzimidazol-2-il]urea.
US8471014B2 (en) 2011-01-14 2013-06-25 Vertex Pharmaceuticals Incorporated Process of making gyrase and topoisomerase IV inhibitors
SG191946A1 (en) 2011-01-14 2013-08-30 Vertex Pharma Pyrimidine gyrase and topoisomerase iv inhibitors
CN103384666A (zh) * 2011-01-14 2013-11-06 沃泰克斯药物股份有限公司 固体形式的促旋酶抑制剂(r)-1-乙基-3-[5-[2-(1-羟基-1-甲基-乙基)嘧啶-5-基]-7-(四氢呋喃-2-基)-1氢-苯并咪唑-2-基]脲
JP5977344B2 (ja) * 2011-06-20 2016-08-24 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated ジャイレースおよびトポイソメラーゼ阻害剤のリン酸エステル
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US9572809B2 (en) * 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
US9018216B2 (en) * 2012-07-18 2015-04-28 Vertex Pharmaceuticals Incorporated Solid forms of (R)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof

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Publication number Publication date
BR112013017974A2 (pt) 2018-05-02
WO2012097269A1 (en) 2012-07-19
AU2012205415B2 (en) 2017-02-02
EP2663557A1 (en) 2013-11-20
CN103443096B (zh) 2016-06-29
AU2012205415A1 (en) 2013-08-01
TWI546298B (zh) 2016-08-21
BR112013017974B1 (pt) 2021-05-25
CN103443096A (zh) 2013-12-11
ZA201305233B (en) 2014-11-26
KR20140037031A (ko) 2014-03-26
NZ612961A (en) 2015-10-30
RU2609259C2 (ru) 2017-01-31
US20120184512A1 (en) 2012-07-19
IL227406A (en) 2017-02-28
US8969359B2 (en) 2015-03-03
US8481551B2 (en) 2013-07-09
ES2545516T3 (es) 2015-09-11
JP6085829B2 (ja) 2017-03-01
AR084863A1 (es) 2013-07-10
SG191946A1 (en) 2013-08-30
CL2013002025A1 (es) 2013-12-27
CA2824516A1 (en) 2012-07-19
MX2013008162A (es) 2013-08-27
EP2663557B1 (en) 2015-05-27
TW201309677A (zh) 2013-03-01
US20130289002A1 (en) 2013-10-31
KR101897952B1 (ko) 2018-09-12
IL227406A0 (en) 2013-09-30
JP2014503557A (ja) 2014-02-13
RU2013137750A (ru) 2015-02-20
CA2824516C (en) 2019-02-26

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