AR084864A1 - Proceso de preparacion de girasa e inhibidores de topoisomerasa iv y compuestos intermediarios de dicho proceso - Google Patents
Proceso de preparacion de girasa e inhibidores de topoisomerasa iv y compuestos intermediarios de dicho procesoInfo
- Publication number
- AR084864A1 AR084864A1 ARP120100138A ARP120100138A AR084864A1 AR 084864 A1 AR084864 A1 AR 084864A1 AR P120100138 A ARP120100138 A AR P120100138A AR P120100138 A ARP120100138 A AR P120100138A AR 084864 A1 AR084864 A1 AR 084864A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- optionally substituted
- compound
- preparation
- girasa
- Prior art date
Links
Classifications
-
- 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
- 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
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/10—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 two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un método para la preparación de un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde R es H o F; y cada uno de R3, R4, y R5 es independientemente un alquilo opcionalmente sustituido, o un grupo hidroxilo opcionalmente protegido: que comprende la provisión de un compuesto de fenilpirimidina de fórmula (2) en donde R es H o F, y cada uno de R3, R4 y R5 es independientemente un alquilo opcionalmente sustituido o un grupo hidroxilo opcionalmente protegido; y la reacción del compuesto de fenilpirimidina de fórmula (2) con un derivado de urea de fórmula (3) ó (4), en donde R6 es un alquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un carbociclo no saturado o saturado opcionalmente sustituido, o un heterociclo no saturado o saturado opcionalmente sustituido para proporcionar un compuesto de fórmula (1); y hacer reaccionar parcialmente el compuesto de formula (1) con un ácido adecuado para proporcionar una sal farmacéuticamente aceptable del compuesto de fórmula (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161432990P | 2011-01-14 | 2011-01-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR084864A1 true AR084864A1 (es) | 2013-07-10 |
Family
ID=45815947
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100138A AR084864A1 (es) | 2011-01-14 | 2012-01-16 | Proceso de preparacion de girasa e inhibidores de topoisomerasa iv y compuestos intermediarios de dicho proceso |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US8471014B2 (es) |
| EP (1) | EP2663556B1 (es) |
| JP (1) | JP6006235B2 (es) |
| KR (1) | KR101882172B1 (es) |
| CN (1) | CN103384665B (es) |
| AR (1) | AR084864A1 (es) |
| AU (1) | AU2012205420B2 (es) |
| BR (1) | BR112013017968B1 (es) |
| CA (1) | CA2824519C (es) |
| ES (1) | ES2526902T3 (es) |
| IL (1) | IL227405B (es) |
| MX (1) | MX355561B (es) |
| NZ (1) | NZ612920A (es) |
| PT (1) | PT2663556E (es) |
| RU (1) | RU2619116C2 (es) |
| SG (1) | SG191945A1 (es) |
| TW (1) | TWI534143B (es) |
| WO (1) | WO2012097274A1 (es) |
| ZA (1) | ZA201305232B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112013017968B1 (pt) * | 2011-01-14 | 2021-03-16 | Spero Therapeutics Inc. | processo para fazer inibidores de girase e de topoisomerase e compostos intermediários |
| 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 |
| WO2012097269A1 (en) * | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | Pyrimidine gyrase and topoisomerase iv inhibitors |
| US8481552B2 (en) * | 2011-01-14 | 2013-07-09 | 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 |
| ES2576298T3 (es) | 2011-06-20 | 2016-07-06 | Vertex Pharmaceuticals Incorporated | Ésteres de fosfato de inhibidores de girasa y topoisomerasa |
| WO2014015105A1 (en) | 2012-07-18 | 2014-01-23 | 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 |
| US9572809B2 (en) | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
| KR20160115986A (ko) | 2014-02-03 | 2016-10-06 | 스페로 자이레이스, 인크 | 폴리믹신을 포함하는 항균성 조합 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US4174400A (en) | 1978-09-13 | 1979-11-13 | Merck & Co., Inc. | Anthelmintic benzimidazoles |
| US4512998A (en) | 1980-10-20 | 1985-04-23 | Schering Corporation | Anthelmintic benzimidazole carbamates |
| CA2028530A1 (en) | 1989-11-21 | 1991-05-22 | Christian Hubschwerlen | Substituted pyrimidobenzimidazole derivatives |
| 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 |
| US5643935A (en) | 1995-06-07 | 1997-07-01 | The University Of North Carolina At Chapel Hill | Method of combatting infectious diseases using dicationic bis-benzimidazoles |
| 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 |
| EP1341769B1 (en) | 2000-12-15 | 2007-10-17 | Vertex Pharmaceuticals Incorporated | Bacterial gyrase inhibitors and uses thereof |
| ES2277088T3 (es) * | 2002-06-13 | 2007-07-01 | Vertex Pharmaceuticals Incorporated | Derivados del acido 2-ureido-6-heteroaril-3h-benzoimidazol-4-carboxilico y compuestos relacionados como inhibidores de girasa y/o topoisomerasa iv para el tratamiento de infecciones bacterianas. |
| US8404852B2 (en) | 2003-01-31 | 2013-03-26 | 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 |
| US7618974B2 (en) | 2003-01-31 | 2009-11-17 | 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 |
| US8193352B2 (en) | 2003-01-31 | 2012-06-05 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| CA2512280A1 (en) * | 2003-03-07 | 2004-09-16 | Kowa Co., Ltd. | Benzofuran derivative |
| CN101321744A (zh) * | 2005-11-07 | 2008-12-10 | 沃泰克斯药物股份有限公司 | 作为回旋酶抑制剂的苯并咪唑衍生物 |
| US8481544B2 (en) | 2006-06-22 | 2013-07-09 | Biota Europe Limited | Antibacterial compositions |
| GB0612428D0 (en) | 2006-06-22 | 2006-08-02 | Prolysis Ltd | Antibacterial agents |
| GB0724349D0 (en) | 2007-12-13 | 2008-01-30 | Prolysis Ltd | Antibacterial agents |
| EP2102199B1 (en) | 2006-12-04 | 2011-04-27 | AstraZeneca AB | Antibacterial polycyclic urea compounds |
| GB0724342D0 (en) | 2007-12-13 | 2008-01-30 | Prolysis Ltd | Anitbacterial compositions |
| WO2009156966A1 (en) | 2008-06-25 | 2009-12-30 | Ranbaxy Laboratories Limited | Benzothiazoles and aza-analogues thereof use as antibacterial agents |
| US9481675B2 (en) | 2009-09-11 | 2016-11-01 | Merck Sharp & Dohme Corp. | Gyrase inhibitors |
| CA2777741A1 (en) | 2009-10-16 | 2011-04-21 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compounds and methods of making and using the same |
| AU2011313820A1 (en) | 2010-10-08 | 2013-04-11 | Biota Europe Ltd | Antibacterial compounds |
| US8481552B2 (en) * | 2011-01-14 | 2013-07-09 | 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 |
| 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 |
| WO2012097269A1 (en) | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | Pyrimidine gyrase and topoisomerase iv inhibitors |
| BR112013017968B1 (pt) | 2011-01-14 | 2021-03-16 | Spero Therapeutics Inc. | processo para fazer inibidores de girase e de topoisomerase e compostos intermediários |
| ES2576298T3 (es) * | 2011-06-20 | 2016-07-06 | Vertex Pharmaceuticals Incorporated | Ésteres de fosfato de inhibidores de girasa y topoisomerasa |
| US8906902B2 (en) | 2012-03-22 | 2014-12-09 | Biota Europe Limited | Antibacterial compounds |
| WO2014015105A1 (en) * | 2012-07-18 | 2014-01-23 | 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 |
| US9572809B2 (en) * | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
-
2012
- 2012-01-13 BR BR112013017968-6A patent/BR112013017968B1/pt active IP Right Grant
- 2012-01-13 PT PT127084168T patent/PT2663556E/pt unknown
- 2012-01-13 JP JP2013549579A patent/JP6006235B2/ja active Active
- 2012-01-13 CA CA2824519A patent/CA2824519C/en active Active
- 2012-01-13 SG SG2013053418A patent/SG191945A1/en unknown
- 2012-01-13 RU RU2013137751A patent/RU2619116C2/ru active
- 2012-01-13 NZ NZ612920A patent/NZ612920A/en unknown
- 2012-01-13 US US13/349,884 patent/US8471014B2/en active Active
- 2012-01-13 KR KR1020137018399A patent/KR101882172B1/ko active IP Right Grant
- 2012-01-13 ES ES12708416.8T patent/ES2526902T3/es active Active
- 2012-01-13 CN CN201280009909.2A patent/CN103384665B/zh active Active
- 2012-01-13 TW TW101101505A patent/TWI534143B/zh active
- 2012-01-13 WO PCT/US2012/021281 patent/WO2012097274A1/en active Application Filing
- 2012-01-13 EP EP12708416.8A patent/EP2663556B1/en active Active
- 2012-01-13 MX MX2013008164A patent/MX355561B/es active IP Right Grant
- 2012-01-13 AU AU2012205420A patent/AU2012205420B2/en active Active
- 2012-01-16 AR ARP120100138A patent/AR084864A1/es active IP Right Grant
-
2013
- 2013-05-28 US US13/903,506 patent/US8912326B2/en active Active
- 2013-07-10 IL IL227405A patent/IL227405B/en active IP Right Grant
- 2013-07-11 ZA ZA2013/05232A patent/ZA201305232B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NZ612920A (en) | 2015-10-30 |
| RU2619116C2 (ru) | 2017-05-12 |
| KR101882172B1 (ko) | 2018-07-26 |
| BR112013017968B1 (pt) | 2021-03-16 |
| US8912326B2 (en) | 2014-12-16 |
| ZA201305232B (en) | 2014-11-26 |
| CA2824519C (en) | 2020-06-16 |
| JP6006235B2 (ja) | 2016-10-12 |
| CA2824519A1 (en) | 2012-07-19 |
| IL227405B (en) | 2018-05-31 |
| KR20140037028A (ko) | 2014-03-26 |
| EP2663556B1 (en) | 2014-10-15 |
| CN103384665B (zh) | 2018-01-09 |
| BR112013017968A2 (pt) | 2016-07-12 |
| AU2012205420B2 (en) | 2016-12-08 |
| TWI534143B (zh) | 2016-05-21 |
| TW201307332A (zh) | 2013-02-16 |
| SG191945A1 (en) | 2013-08-30 |
| IL227405A0 (en) | 2013-09-30 |
| EP2663556A1 (en) | 2013-11-20 |
| MX355561B (es) | 2018-04-23 |
| US8471014B2 (en) | 2013-06-25 |
| PT2663556E (pt) | 2014-11-27 |
| JP2014503558A (ja) | 2014-02-13 |
| WO2012097274A1 (en) | 2012-07-19 |
| US20130261305A1 (en) | 2013-10-03 |
| AU2012205420A1 (en) | 2013-08-01 |
| MX2013008164A (es) | 2013-08-27 |
| US20120184742A1 (en) | 2012-07-19 |
| ES2526902T3 (es) | 2015-01-16 |
| RU2013137751A (ru) | 2015-02-20 |
| CN103384665A (zh) | 2013-11-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |