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
Links
- 108010041052 DNA Topoisomerase IV Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 230000001580 bacterial effect Effects 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000002110 toxicologic effect Effects 0.000 abstract 1
- 231100000723 toxicological property Toxicity 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic 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
- C07F9/65586—Heterocyclic 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.
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) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8471014B2 (en) | 2011-01-14 | 2013-06-25 | Vertex Pharmaceuticals Incorporated | Process of making gyrase and topoisomerase IV inhibitors |
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 |
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 |
SG11201606332PA (en) | 2014-02-03 | 2016-09-29 | Spero Gyrase Inc | Antibacterial combinations comprising polymyxin |
AU2017291826B2 (en) * | 2016-07-07 | 2021-10-21 | Cyclerion Therapeutics, Inc. | Phosphorus prodrugs of sGC stimulators |
WO2018174288A1 (ja) | 2017-03-24 | 2018-09-27 | 大正製薬株式会社 | 2(1h)-キノリノン誘導体 |
US20200345637A1 (en) * | 2018-01-19 | 2020-11-05 | Aiviva Biopharma, Inc. | Suspension compositions of multi-target inhibitors |
CN109464472B (zh) * | 2019-01-17 | 2023-09-15 | 广西医科大学 | 一种铜绿假单胞菌家兔脓胸引流管生物膜模型建立方法 |
CN109464471B (zh) * | 2019-01-17 | 2023-09-19 | 广西医科大学 | 一种铜绿假单胞菌家兔脓胸脓絮状物生物膜模型建立方法 |
WO2023076369A1 (en) * | 2021-10-26 | 2023-05-04 | Spero Therapeutics, Inc. | Human efficacious dose and dosage schedule of spr720 |
WO2024112738A1 (en) * | 2022-11-22 | 2024-05-30 | University Of Maryland, Baltimore | Bovine colostrum-derived nutritional supplements and uses thereof |
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AR042956A1 (es) | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
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 |
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US8404852B2 (en) | 2003-01-31 | 2013-03-26 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
CN101171247A (zh) * | 2005-03-04 | 2008-04-30 | 阿斯利康(瑞典)有限公司 | 作为dna促旋酶和拓扑异构酶抑制剂的吡咯衍生物 |
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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 |
US9604976B2 (en) | 2012-03-22 | 2017-03-28 | Spero Gyrase, Inc. | Antibacterial compounds |
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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2012
- 2012-01-13 SG SG2013053426A patent/SG191946A1/en unknown
- 2012-01-13 JP JP2013549575A patent/JP6085829B2/ja active Active
- 2012-01-13 MX MX2013008162A patent/MX339455B/es active IP Right Grant
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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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