CO5251401A1 - Inhibidores de fab i - Google Patents
Inhibidores de fab iInfo
- Publication number
- CO5251401A1 CO5251401A1 CO00076101A CO00076101A CO5251401A1 CO 5251401 A1 CO5251401 A1 CO 5251401A1 CO 00076101 A CO00076101 A CO 00076101A CO 00076101 A CO00076101 A CO 00076101A CO 5251401 A1 CO5251401 A1 CO 5251401A1
- Authority
- CO
- Colombia
- Prior art keywords
- 4alkyl
- het
- fab
- inhibitors
- 6alkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- 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
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Semiconductor Lasers (AREA)
- Indole Compounds (AREA)
Abstract
Un compuesto de la fórmula (I):<EMI FILE="00076101_1" ID="1" IMF=JPEG >donde: R1 es alquilo C1-4; R2 es alquilo C1-4; R3 es -alquilo C1-4, -alquil C0-4-Ar, o -alquil C0-4-Het; R4 es -alquilo C1-4, -(CH2)1-4OH, -O-alquilo C1-4, -S-alquilo C1-4, -N(alquilo C1-4)2, -alquil C0-4-Ar, -alquil C0-4 -Het, -alquil C0-4-cicloalquilo C3-6, -CH(OH)-CH2-R* o -(CH2)1-3SOzAr; R* es alquilo C1-4, Ar o Het; X es H, alquilo C1-4, ORAND#39, SRAND#39, CN, N(RAND#39)2, CH2N(RAND#39)2, NO2, CF3, CO2RAND#39, CON(R')2, CORAND#39, NRAND#39C(O)RAND#39, F, Cl, Br, I, o -S(O)r CF3; RAND#39 es H, alquilo C 1-6, -alquil C0-4 -Ar; y r es 0, 1 ó 2;o una de sus sales farmacéuticamente aceptables.1 Un procedimiento para preparar un compuesto de la fórmula (I) como se define en la reivindicación 1, cuyo procedimiento comprende hacer reaccionar un compuesto de la fórmula (II) con un compuesto de la fórmula (III): <EMI FILE="00076101_2" ID="2" IMF=JPEG >donde R1, R2, R3, R4 y X son como se han definido en la fórmula (I), con todos los grupos funcionales reactivos protegidos, en presencia de EDC y HOBt; y separar después todos los grupos protectores, y opcionalmente formar una sal farmacéuticamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15852999P | 1999-10-08 | 1999-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5251401A1 true CO5251401A1 (es) | 2003-02-28 |
Family
ID=22568552
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00076101A CO5251401A1 (es) | 1999-10-08 | 2000-10-06 | Inhibidores de fab i |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1225895B1 (es) |
| JP (1) | JP4961084B2 (es) |
| AT (1) | ATE294578T1 (es) |
| AU (1) | AU1192501A (es) |
| CO (1) | CO5251401A1 (es) |
| DE (1) | DE60019954T2 (es) |
| HK (1) | HK1049610A1 (es) |
| WO (1) | WO2001026654A1 (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CO5180550A1 (es) | 1999-04-19 | 2002-07-30 | Smithkline Beecham Corp | Inhibidores de fab i |
| CO5370679A1 (es) | 1999-06-01 | 2004-02-27 | Smithkline Beecham Corp | Inhibidores fab 1 |
| CA2387016C (en) | 1999-10-08 | 2010-09-28 | William H. Miller | Acrylamide derivatives as fab i inhibitors |
| AU7866300A (en) * | 1999-10-08 | 2001-04-23 | Smithkline Beecham Corporation | Fab i inhibitors |
| US6730684B1 (en) * | 1999-10-08 | 2004-05-04 | Affinium Pharmaceuticals, Inc. | Fab I inhibitors |
| US6762201B1 (en) | 1999-10-08 | 2004-07-13 | Affinium Pharmaceuticals, Inc. | Fab I inhibitors |
| CA2425185A1 (en) * | 2000-10-06 | 2002-04-11 | Stephane De Lombaert | Benzimidazole and indole derivatives as crf receptor modulators |
| WO2003088897A2 (en) | 2001-04-06 | 2003-10-30 | Affinium Pharmaceuticals, Inc. | Fab i inhibitors |
| EP1575951B1 (en) * | 2002-12-06 | 2014-06-25 | Debiopharm International SA | Heterocyclic compounds, methods of making them and their use in therapy |
| WO2004082586A2 (en) * | 2003-03-17 | 2004-09-30 | Affinium Pharmaceuticals, Inc. | Phamaceutical compositions comprising inhibitors of fab i and further antibiotics |
| CN101203504B (zh) * | 2005-05-03 | 2012-11-14 | 兰贝克赛实验室有限公司 | 抗微生物剂 |
| CA2606804A1 (en) | 2005-05-03 | 2006-11-09 | Ranbaxy Laboratories Limited | Antimicrobial agents |
| JP2009533315A (ja) * | 2006-04-10 | 2009-09-17 | ランバクシー ラボラトリーズ リミテッド | 抗菌剤 |
| EP2054422B1 (en) | 2006-07-20 | 2017-06-14 | Debiopharm International SA | Acrylamide derivatives as fab i inhibitors |
| EP3255045A1 (en) | 2007-02-16 | 2017-12-13 | Debiopharm International SA | Salts, prodrugs and polymorphs of fab i inhibitors |
| JO3611B1 (ar) | 2011-08-10 | 2020-08-27 | Janssen Sciences Ireland Uc | سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم |
| KR101996866B1 (ko) | 2011-08-10 | 2019-07-05 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 항균성 호모피페리디닐 치환 3,4-디하이드로-1h-[1,8]나프티리디논 |
| US9012634B2 (en) | 2011-08-10 | 2015-04-21 | Janssen R&D Ireland | Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones |
| JP6085026B2 (ja) | 2012-06-19 | 2017-02-22 | デビオファーム インターナショナル エスエーＤｅｂｉｏｐｈａｒｍ Ｉｎｔｅｒｎａｔｉｏｎａｌ Ｓａ | （ｅ）−ｎ−メチル−ｎ−（（３−メチルベンゾフラン−２−イル）メチル）−３−（７−オキソ−５，６，７，８−テトラヒドロ−１，８−ナフチリジン−３−イル）アクリルアミドのプロドラッグ誘導体 |
| AU2013301452B2 (en) | 2012-08-10 | 2017-06-01 | Janssen Sciences Ireland Uc | New antibacterial compounds |
| EA201590339A1 (ru) | 2012-08-10 | 2015-06-30 | Янссен Сайенсиз Айрлэнд Юси | Новые антибактериальные соединения |
| US10751351B2 (en) | 2016-02-26 | 2020-08-25 | Debiopharm International S.A. | Medicament for treatment of diabetic foot infections |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6207679B1 (en) * | 1997-06-19 | 2001-03-27 | Sepracor, Inc. | Antimicrobial agents uses and compositions related thereto |
| US5932743A (en) * | 1997-08-21 | 1999-08-03 | American Home Products Corporation | Methods for the solid phase synthesis of substituted indole compounds |
-
2000
- 2000-10-06 DE DE60019954T patent/DE60019954T2/de not_active Expired - Lifetime
- 2000-10-06 WO PCT/US2000/027591 patent/WO2001026654A1/en active IP Right Grant
- 2000-10-06 AU AU11925/01A patent/AU1192501A/en not_active Abandoned
- 2000-10-06 AT AT00973420T patent/ATE294578T1/de not_active IP Right Cessation
- 2000-10-06 EP EP00973420A patent/EP1225895B1/en not_active Expired - Lifetime
- 2000-10-06 JP JP2001529444A patent/JP4961084B2/ja not_active Expired - Fee Related
- 2000-10-06 CO CO00076101A patent/CO5251401A1/es not_active Application Discontinuation
-
2003
- 2003-01-14 HK HK03100340.4A patent/HK1049610A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP4961084B2 (ja) | 2012-06-27 |
| EP1225895B1 (en) | 2005-05-04 |
| WO2001026654A1 (en) | 2001-04-19 |
| HK1049610A1 (zh) | 2003-05-23 |
| DE60019954T2 (de) | 2006-02-23 |
| EP1225895A4 (en) | 2002-11-13 |
| ATE294578T1 (de) | 2005-05-15 |
| JP2003511415A (ja) | 2003-03-25 |
| EP1225895A1 (en) | 2002-07-31 |
| DE60019954D1 (en) | 2005-06-09 |
| AU1192501A (en) | 2001-04-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Application withdrawn |