CO5180550A1 - Inhibidores de fab i - Google Patents
Inhibidores de fab iInfo
- Publication number
- CO5180550A1 CO5180550A1 CO00027745A CO00027745A CO5180550A1 CO 5180550 A1 CO5180550 A1 CO 5180550A1 CO 00027745 A CO00027745 A CO 00027745A CO 00027745 A CO00027745 A CO 00027745A CO 5180550 A1 CO5180550 A1 CO 5180550A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- knr
- co2r
- cycloalkyl
- oxoalkynyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- -1 R2 is H Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005021 aminoalkenyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000005014 aminoalkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Abstract
Un compuesto de la fórmula (I)<EMI FILE="00027745_1" ID="1" IMF=JPEG >donde:R1 es H, alquilo C1-6 o Ar-alquilo C0-6,R2 es H, alquilo C1-6, Ar-alquilo C0-6, HO-(CH2)n- o R´OC(O)-(CH2)n-; R3 es A-alquilo C0-4, A-alquenilo C2-4, A-alquinilo C2-4, A-oxoalquinilo C3-4, oxoalquinilo C3-4, A-aminoalquilo C1-4, A-aminoalquenilo C3-4, A-aminoalquiniloC3-4, opcionalmente sustituidos con cualquier combinación accessible de uno o más de R10 o R7;R4 es<EMI FILE="00027745_2" ID="2" IMF=JPEG >R5 es H, alquilo C1-6, Ar-alquilo C0-6, o cicloalquilo C3-6-alquilo C0-6;A es H, cicloalquilo C3-6, Het o Ar;R7 es -COR8, -COCR´2R9, -C(S)R8, -S(O)kOR´, -S(O)kNR´R", -PO(OR´), -PO(OR´)2, -B(OR´)2, -NO2, o tetrazolilo;R8 es -OR´, -NR´R", -NR´SO2R´, -NR´OR´, o -OCR´2CO(O)R´;R9 es -OR´, -CN, -S(O)rR´, -S(O)kNR´2, -C(O)R´, C(O)NR´2, o -CO2R´;R10 es H, halo, -OR11, -CN, -NR´R11, -NO2, -CF3, CF3S(O)r-, -CO2R´, -CONR´2, A-alquil C0-6, A-oxoalquil C1-6-, A-alquenil C2-6-, A-alquinil C2-6-, A-alquiloxi C0-6-, A-alquil C0-6-amino- o A-alquil C0-6-S(O)r-;R11 es R´, -C(O)R´, -C(O)NR´2, -C(O)OR´, -S(O)kR´, o -S(O)kNR´2;R´ es H, alquilo C1-6, Ar-alquilo C0-6, o cicloalquilo C3-6-alquilo C0-6;R" es R´, -C(O)R´ o -C(O)OR´;R"´ es H, alquilo C1-6, Ar-alquilo C0-6, HO-(CH2)2-, R´C(O)-, (R´)2NC(O)CH2- oR´S(O)2-;X es H, alquilo C1-4, OR´, SR´, alquil C1-4-sulfonilo, alquil C1-4-sulfoxilo, -CN, N(R´)2, CH2N(R´)2, -NO2, -CF3, -CO2R´, -CON(R´)2, -COR´, -NR´C(O)R´, F, Cl, Br, I, o CF3S(O)r-;k es 1 ó 2;m es 1 , 2 ó 3n es, de 1 a 6; yr es 0, 1 ó 2;o una de sus sales farmacéuticamente aceptables.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12992899P | 1999-04-19 | 1999-04-19 | |
| US13010199P | 1999-04-20 | 1999-04-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5180550A1 true CO5180550A1 (es) | 2002-07-30 |
Family
ID=26828036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00027745A CO5180550A1 (es) | 1999-04-19 | 2000-04-14 | Inhibidores de fab i |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US6503903B1 (es) |
| EP (1) | EP1171428B1 (es) |
| JP (1) | JP4647791B2 (es) |
| AT (1) | ATE433963T1 (es) |
| AU (1) | AU4652000A (es) |
| CO (1) | CO5180550A1 (es) |
| DE (1) | DE60042401D1 (es) |
| WO (1) | WO2000063187A1 (es) |
Families Citing this family (23)
| 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 |
| CO5251397A1 (es) * | 1999-10-08 | 2003-02-28 | Smithkline Beecham Corp | Inhibidores de fab i |
| EP1226138B1 (en) * | 1999-10-08 | 2004-12-29 | Affinium Pharmaceuticals, Inc. | 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 |
| WO2003088897A2 (en) * | 2001-04-06 | 2003-10-30 | Affinium Pharmaceuticals, Inc. | Fab i inhibitors |
| FR2835186B1 (fr) | 2002-01-28 | 2006-10-20 | Aventis Pharma Sa | Nouveaux composes heterocycliques, actifs comme inhibiteurs de beta-lactamases |
| FR2844273B1 (fr) | 2002-09-05 | 2008-04-04 | Aventis Pharma Sa | Nouveaux composes heterocycliques, procede et intermediaires de preparation et utilisation comme medicament, notamment comme inhibiteurs de beta-lactamases et anti-bacteriens. |
| EP1575951B1 (en) * | 2002-12-06 | 2014-06-25 | Debiopharm International SA | Heterocyclic compounds, methods of making them and their use in therapy |
| US7439253B2 (en) | 2002-12-06 | 2008-10-21 | Novexel | Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors |
| FR2848210B1 (fr) * | 2002-12-06 | 2007-10-19 | Aventis Pharma Sa | Nouveaux composes heterocycliques, leur preparation et leur utilisation comme medicaments, notamment comme anti-bacteriens et inhibiteurs de beta-lactamases |
| CA2519429C (en) * | 2003-03-17 | 2013-08-06 | Affinium Pharmaceuticals, Inc. | Pharmaceutical compositions comprising inhibitors of fab i and further antibiotics |
| PT1828167E (pt) * | 2004-06-04 | 2014-10-08 | Debiopharm Int Sa | Derivados de acrilamida como agentes antibióticos |
| FR2880625B1 (fr) * | 2005-01-07 | 2007-03-09 | Sanofi Aventis Sa | Derives de n-(heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique |
| EP1973902A2 (en) * | 2005-12-05 | 2008-10-01 | Affinium Pharmaceuticals, Inc. | 3-heterocyclylacrylamide compounds as fabi inhibitors and antibacterial agents |
| JP5468899B2 (ja) | 2006-07-20 | 2014-04-09 | アフィニウム ファーマシューティカルズ， インク． | Ｆａｂｉインヒビターとしてのアクリルアミド誘導体 |
| WO2008098374A1 (en) | 2007-02-16 | 2008-08-21 | Affinium Pharmaceuticals, Inc. | Salts, prodrugs and polymorphs of fab i inhibitors |
| MY165902A (en) | 2011-12-02 | 2018-05-18 | Aurigene Discovery Tech Ltd | Substituted pyridine derivatives as fabi inhibitors |
| US9062075B2 (en) | 2011-12-02 | 2015-06-23 | Aurigene Discovery Technologies Limited | Tetrahydropyridine derivatives as FabI inhibitors |
| BR112014031635B1 (pt) | 2012-06-19 | 2022-01-11 | Debiopharm International Sa | Derivados de pró-fármaco de (e)-n-metil-n-( (3-metilbenzofuran-2-il) metil)-3-(7-oxo-5,6,7,8- tetraidro- 1, 8- naftirindin-3-il) acrilamida |
| EP3004099B1 (en) | 2013-06-04 | 2023-04-19 | Aurigene Oncology Limited | Tetrahydropyridine derivatives as fabi inhibitors |
| CN108778286A (zh) | 2016-02-26 | 2018-11-09 | 德彪药业国际股份公司 | 用于治疗糖尿病足感染的药物 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3828068A (en) | 1971-05-10 | 1974-08-06 | Tenneco Chem | ((substituted indazolyl)-n1-methyl)carbamates |
| US4154943A (en) | 1977-12-29 | 1979-05-15 | University Of Vermont | Preparation of vincadifformine |
| FR2619111B1 (fr) | 1987-08-07 | 1991-01-11 | Synthelabo | Derives de (piperidinyl-4)methyl-2 tetrahydro-1,2,3,4 9h-pyrido (3,4-b) indole, leur preparation et leur application en therapeutique |
| EP0593603B1 (en) | 1991-06-28 | 2002-11-20 | Smithkline Beecham Corporation | Bicyclic fibrinogen antagonists |
| FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| CN1041921C (zh) | 1992-12-21 | 1999-02-03 | 史密丝克莱恩比彻姆公司 | 双环血纤维蛋白原拮抗剂 |
| MA23420A1 (fr) * | 1994-01-07 | 1995-10-01 | Smithkline Beecham Corp | Antagonistes bicycliques de fibrinogene. |
| US5614551A (en) | 1994-01-24 | 1997-03-25 | The Johns Hopkins University | Inhibitors of fatty acid synthesis as antimicrobial agents |
| CN1156995A (zh) * | 1994-06-29 | 1997-08-13 | 史密丝克莱恩比彻姆公司 | 玻璃体结合蛋白受体拮抗剂 |
| DE19624659A1 (de) | 1996-06-20 | 1998-01-08 | Klinge Co Chem Pharm Fab | Neue Pyridylalken- und Pyridylalkinsäureamide |
| US6451816B1 (en) | 1997-06-20 | 2002-09-17 | Klinge Pharma Gmbh | Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression |
| AU6870098A (en) | 1997-03-31 | 1998-10-22 | Du Pont Merck Pharmaceutical Company, The | Indazoles of cyclic ureas useful as hiv protease inhibitors |
| US6207679B1 (en) | 1997-06-19 | 2001-03-27 | Sepracor, Inc. | Antimicrobial agents uses and compositions related thereto |
| EP1007051A4 (en) * | 1997-08-04 | 2001-08-29 | Smithkline Beecham Corp | INTEGRIN RECEPTOR ANTAGONISTS |
| US5932743A (en) | 1997-08-21 | 1999-08-03 | American Home Products Corporation | Methods for the solid phase synthesis of substituted indole compounds |
| CO5180550A1 (es) | 1999-04-19 | 2002-07-30 | Smithkline Beecham Corp | Inhibidores de fab i |
| AR024077A1 (es) | 1999-05-25 | 2002-09-04 | Smithkline Beecham Corp | Compuestos antibacterianos |
| CO5370679A1 (es) | 1999-06-01 | 2004-02-27 | Smithkline Beecham Corp | Inhibidores fab 1 |
| CO5180605A1 (es) | 1999-06-23 | 2002-07-30 | Smithkline Beecham Corp | Compuestos de indol |
| US6346391B1 (en) | 1999-07-22 | 2002-02-12 | Trustees Of Tufts College | Methods of reducing microbial resistance to drugs |
| EP1225895B1 (en) | 1999-10-08 | 2005-05-04 | Affinium Pharmaceuticals, Inc. | Fab i inhibitors |
| EP1226138B1 (en) | 1999-10-08 | 2004-12-29 | Affinium Pharmaceuticals, Inc. | Fab i inhibitors |
| CO5251397A1 (es) | 1999-10-08 | 2003-02-28 | Smithkline Beecham Corp | Inhibidores de fab i |
| US6503908B1 (en) | 1999-10-11 | 2003-01-07 | Pfizer Inc | Pharmaceutically active compounds |
| US6656703B1 (en) | 1999-12-29 | 2003-12-02 | Millennium Pharamaceuticals, Inc. | High throughput screen for inhibitors of fatty acid biosynthesis in bacteria |
| US6372752B1 (en) | 2000-02-07 | 2002-04-16 | Genzyme Corporation | Inha inhibitors and methods of use thereof |
| US6642252B2 (en) | 2000-11-07 | 2003-11-04 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| US20020107266A1 (en) | 2000-12-12 | 2002-08-08 | Marguerita Lim-Wilby | Compounds, compositions and methods for treatment of parasitic infections |
-
2000
- 2000-04-14 CO CO00027745A patent/CO5180550A1/es unknown
- 2000-04-19 DE DE60042401T patent/DE60042401D1/de not_active Expired - Lifetime
- 2000-04-19 AU AU46520/00A patent/AU4652000A/en not_active Abandoned
- 2000-04-19 AT AT00928259T patent/ATE433963T1/de not_active IP Right Cessation
- 2000-04-19 EP EP00928259A patent/EP1171428B1/en not_active Expired - Lifetime
- 2000-04-19 WO PCT/US2000/010695 patent/WO2000063187A1/en active Application Filing
- 2000-04-19 JP JP2000612279A patent/JP4647791B2/ja not_active Expired - Fee Related
-
2001
- 2001-10-18 US US09/959,172 patent/US6503903B1/en not_active Expired - Lifetime
-
2002
- 2002-11-12 US US10/292,687 patent/US6765005B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1171428A4 (en) | 2004-09-15 |
| US6765005B2 (en) | 2004-07-20 |
| EP1171428A1 (en) | 2002-01-16 |
| ATE433963T1 (de) | 2009-07-15 |
| DE60042401D1 (de) | 2009-07-30 |
| EP1171428B1 (en) | 2009-06-17 |
| US20030139377A1 (en) | 2003-07-24 |
| AU4652000A (en) | 2000-11-02 |
| US6503903B1 (en) | 2003-01-07 |
| JP2002542235A (ja) | 2002-12-10 |
| JP4647791B2 (ja) | 2011-03-09 |
| WO2000063187A1 (en) | 2000-10-26 |
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