MX2013008161A - 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. - Google Patents
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.Info
- Publication number
- MX2013008161A MX2013008161A MX2013008161A MX2013008161A MX2013008161A MX 2013008161 A MX2013008161 A MX 2013008161A MX 2013008161 A MX2013008161 A MX 2013008161A MX 2013008161 A MX2013008161 A MX 2013008161A MX 2013008161 A MX2013008161 A MX 2013008161A
- Authority
- MX
- Mexico
- Prior art keywords
- ethyl
- solid forms
- ydroxy
- benzimidazol
- pyrimidin
- Prior art date
Links
- 239000007787 solid Substances 0.000 title abstract 2
- BKUISYCLLXCBJV-CQSZACIVSA-N 1-ethyl-3-[5-fluoro-6-[2-(2-hydroxypropan-2-yl)pyrimidin-5-yl]-4-[(2r)-oxolan-2-yl]-1h-benzimidazol-2-yl]urea Chemical compound C=12NC(NC(=O)NCC)=NC2=CC(C=2C=NC(=NC=2)C(C)(C)O)=C(F)C=1[C@H]1CCCO1 BKUISYCLLXCBJV-CQSZACIVSA-N 0.000 title 1
- 239000002271 gyrase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 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
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- 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
- A61K31/41—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
-
- A—HUMAN NECESSITIES
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- 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
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Otolaryngology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente solicitud se dirige a formas sólidas de compuestos de la fórmula (I) y sales farmacéuticamente aceptables de la misma, que inhiben la girasa y/o Topo IV bacterianas y composiciones farmacéuticas que comprende los compuestos y sales. Estos compuestos y sales son útiles en el tratamiento de infecciones bacterianas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161433169P | 2011-01-14 | 2011-01-14 | |
| PCT/US2012/021280 WO2012097273A1 (en) | 2011-01-14 | 2012-01-13 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013008161A true MX2013008161A (es) | 2013-08-27 |
| MX341342B MX341342B (es) | 2016-08-17 |
Family
ID=45558414
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013008161A MX341342B (es) | 2011-01-14 | 2012-01-13 | 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. |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US8476281B2 (es) |
| EP (1) | EP2663562B1 (es) |
| JP (1) | JP6120775B2 (es) |
| KR (1) | KR101900249B1 (es) |
| CN (1) | CN103403000B (es) |
| AR (1) | AR085308A1 (es) |
| AU (1) | AU2012205419B2 (es) |
| BR (1) | BR112013017985B1 (es) |
| CA (1) | CA2824403C (es) |
| CL (1) | CL2013002027A1 (es) |
| ES (1) | ES2705923T3 (es) |
| IL (1) | IL227408B (es) |
| MX (1) | MX341342B (es) |
| RU (1) | RU2625305C2 (es) |
| SG (1) | SG191927A1 (es) |
| TW (1) | TWI535714B (es) |
| WO (1) | WO2012097273A1 (es) |
| ZA (1) | ZA201305231B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG191946A1 (en) * | 2011-01-14 | 2013-08-30 | Vertex Pharma | Pyrimidine gyrase and topoisomerase iv inhibitors |
| WO2012097270A1 (en) * | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | 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 |
| CA2824519C (en) * | 2011-01-14 | 2020-06-16 | Vertex Pharmaceuticals Incorporated | Process of making gyrase and topoisomerase inhibitors |
| TWI535714B (zh) * | 2011-01-14 | 2016-06-01 | 維泰克斯製藥公司 | 旋轉酶抑制劑(r)-1-乙基-3-[6-氟-5-[2-(1-羥基-1-甲基-乙基)嘧啶-5-基]-7-(四氫呋喃-2-基)-1h-苯并咪唑-2-基]脲之固體形式 |
| EP2721026B1 (en) | 2011-06-20 | 2016-03-02 | Vertex Pharmaceuticals Incorporated | Phosphate esters of gyrase and topoisomerase inhibitors |
| AR093226A1 (es) | 2012-07-18 | 2015-05-27 | Vertex Pharma | Formas solidas de dihidrogeno fosfato de (r)-2-(5-(2-(3-etilureido)-6-fluoro-7-(tetrahidrofuran-2-il)-1h-benzo[d]imidazol-5-il)pirimidin-2-il)propan-2-ilo y sus sales |
| US9572809B2 (en) | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
| WO2015114452A2 (en) | 2014-02-03 | 2015-08-06 | Biota Europe Ltd | Antibacterial compounds |
| TWI732337B (zh) * | 2014-06-20 | 2021-07-01 | 美商梅琳塔有限責任公司 | 醫藥組成物及其用途 |
| CA3092315C (en) * | 2018-03-05 | 2023-08-29 | Jian Xiong | Crystal form and salt form of pyridopyrazole compound and preparation method therefor |
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| DE2015676A1 (de) | 1970-04-02 | 1971-10-21 | Farbenfabriken Bayer Ag, 5090 Leverkusen | Neue Imine der 2-Formyl-chinoxalindi-N-oxidcarbon-säure-(3) und deren Salze, Verfahren zu ihrer Herstellung und ihre Verwendung als antimikrobielle Mittel |
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| US4512998A (en) | 1980-10-20 | 1985-04-23 | Schering Corporation | Anthelmintic benzimidazole carbamates |
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| 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 |
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| US7727992B2 (en) | 2002-06-13 | 2010-06-01 | 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 |
| US8404852B2 (en) | 2003-01-31 | 2013-03-26 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7618974B2 (en) | 2003-01-31 | 2009-11-17 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| AR042956A1 (es) | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
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| WO2012097270A1 (en) * | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | 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 |
| SG191946A1 (en) * | 2011-01-14 | 2013-08-30 | Vertex Pharma | Pyrimidine gyrase and topoisomerase iv inhibitors |
| CA2824519C (en) * | 2011-01-14 | 2020-06-16 | Vertex Pharmaceuticals Incorporated | Process of making gyrase and topoisomerase inhibitors |
| TWI535714B (zh) * | 2011-01-14 | 2016-06-01 | 維泰克斯製藥公司 | 旋轉酶抑制劑(r)-1-乙基-3-[6-氟-5-[2-(1-羥基-1-甲基-乙基)嘧啶-5-基]-7-(四氫呋喃-2-基)-1h-苯并咪唑-2-基]脲之固體形式 |
| EP2721026B1 (en) * | 2011-06-20 | 2016-03-02 | Vertex Pharmaceuticals Incorporated | Phosphate esters of gyrase and topoisomerase inhibitors |
| JP2015514063A (ja) | 2012-03-22 | 2015-05-18 | ビオタ ヨーロッパ リミテッドBiota Europe Ltd | 抗菌化合物 |
| AR093226A1 (es) * | 2012-07-18 | 2015-05-27 | Vertex Pharma | Formas solidas de dihidrogeno fosfato de (r)-2-(5-(2-(3-etilureido)-6-fluoro-7-(tetrahidrofuran-2-il)-1h-benzo[d]imidazol-5-il)pirimidin-2-il)propan-2-ilo y sus sales |
| US9572809B2 (en) * | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
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2012
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- 2012-01-13 SG SG2013053186A patent/SG191927A1/en unknown
- 2012-01-13 EP EP12701811.7A patent/EP2663562B1/en active Active
- 2012-01-13 CN CN201280009901.6A patent/CN103403000B/zh active Active
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- 2012-01-13 RU RU2013137752A patent/RU2625305C2/ru active
- 2012-01-13 WO PCT/US2012/021280 patent/WO2012097273A1/en not_active Ceased
- 2012-01-13 US US13/349,984 patent/US8476281B2/en active Active
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| CL2013002027A1 (es) | 2013-12-13 |
| IL227408A0 (en) | 2013-09-30 |
| ES2705923T3 (es) | 2019-03-27 |
| WO2012097273A1 (en) | 2012-07-19 |
| CN103403000A (zh) | 2013-11-20 |
| CN103403000B (zh) | 2017-05-31 |
| AR085308A1 (es) | 2013-09-25 |
| NZ612918A (en) | 2015-10-30 |
| BR112013017985B1 (pt) | 2021-06-29 |
| ZA201305231B (en) | 2014-11-26 |
| US20130267540A1 (en) | 2013-10-10 |
| JP2014502640A (ja) | 2014-02-03 |
| JP6120775B2 (ja) | 2017-04-26 |
| US8476281B2 (en) | 2013-07-02 |
| CA2824403A1 (en) | 2012-07-19 |
| MX341342B (es) | 2016-08-17 |
| SG191927A1 (en) | 2013-08-30 |
| AU2012205419A1 (en) | 2013-08-01 |
| EP2663562A1 (en) | 2013-11-20 |
| EP2663562B1 (en) | 2018-11-07 |
| TW201309678A (zh) | 2013-03-01 |
| US20120184564A1 (en) | 2012-07-19 |
| TWI535714B (zh) | 2016-06-01 |
| RU2625305C2 (ru) | 2017-07-13 |
| BR112013017985A2 (pt) | 2019-10-01 |
| US9040542B2 (en) | 2015-05-26 |
| KR20140037030A (ko) | 2014-03-26 |
| CA2824403C (en) | 2019-09-24 |
| KR101900249B1 (ko) | 2018-11-02 |
| IL227408B (en) | 2018-04-30 |
| AU2012205419B2 (en) | 2016-12-15 |
| RU2013137752A (ru) | 2015-02-20 |
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