AR044512A1 - Fenil acetamidas sustituidas, y su utilizacion como inhibidores de las proteasas - Google Patents
Fenil acetamidas sustituidas, y su utilizacion como inhibidores de las proteasasInfo
- Publication number
- AR044512A1 AR044512A1 ARP040101198A ARP040101198A AR044512A1 AR 044512 A1 AR044512 A1 AR 044512A1 AR P040101198 A ARP040101198 A AR P040101198A AR P040101198 A ARP040101198 A AR P040101198A AR 044512 A1 AR044512 A1 AR 044512A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- halogen
- alkoxy
- hydroxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C291/00—Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/00 - C07C281/00
- C07C291/02—Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/00 - C07C281/00 containing nitrogen-oxide bonds
- C07C291/04—Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/00 - C07C281/00 containing nitrogen-oxide bonds containing amino-oxide bonds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/26—Radicals substituted by halogen atoms or nitro radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Abstract
Se describen compuestos de fenilacetamida, o un solvato, o hidrato farmacéuticamente aceptables de los mismos. Los compuestos de la presente son potentes inhibidores de las proteasas, especialmente la serina proteasa de tipo tripsina, tales como la trombina y el factor Xa. Se revelan composiciones para inhibir la pérdida de las plaquetas sanguíneas, inhibir la formación de agregados de las plaquetas sanguíneas, inhibir la formación de la trombina, inhibir la formación de la fibrina, inhibir la formación de trombos, e inhibir la formación de émbolos. Otros usos de los compuestos de la invención es como anticoagulantes sea embebidos en sea físicamente ligados a los materiales utilizados en la manufactura de los dispositivos utilizados en la recolección de la sangre, circulación de la sangre, y almacenamiento de la sangre tales como catéteres, máquinas para la diálisis de la sangre, jeringas y tubos para la recolección de la sangre, tuberías de sangre y stents. Adicionalmente, los compuestos pueden ser etiquetados de manera detectable y utilizados para la formación de imágenes in vivo de los trombos. Reivindicación 1: Un compuesto de la fórmula (1), o un solvato, hidrato o sal farmacéuticamente aceptable de los mismos; en donde: W es R1 o R1S(O2); R1 es R2; R2(CH2)tC(R12)2, donde t es 0-3, y cada uno de los R12 puede ser igual o diferente; (R2)(OR12)CH(CH2)p, donde p es 1-4, (R2)2(OR12)C(CH2)p, donde p es 1-4, R2C(R12)2(CH2)t, en donde t es 0-3, y cada uno de los R12 puede ser igual o diferente, en donde (R12)2 también puede formar un anillo con C representado por cicloalquilo C3-9; R2CF2C(R12)2(CH2)q, en donde q es 0-2, y cada uno de los R12 puede ser igual o diferente, en donde (R12)2 también puede formar un anillo con C representado por cicloalquilo C3-9, R2CH2C(R12)2(CH2)q, en donde q es 0-2, y cada uno de los R12 puede ser igual o diferente, en donde (R12)2 también puede formar un anillo con C representado por cicloalquilo C3-9, (R2)2CH(CH2)r, donde r es 0-4 y cada uno de los R2 puede ser igual o diferente, y en donde (R2)2 también puede formar un anillo con CH representado por cicloalquilo C3-9, alquilo bicíclico C7-12, alquilo tricíclico C10-16, o un anillo heterocíclico mono- o bicíclico de 5- a 7 miembros que puede estar saturado o insaturado, y que contiene de uno a tres heteroátomos seleccionados entre el grupo consistente en N, O y S; R2O(CH2)p, en donde p es 2-4, (R2)2CF(CH2)r, en donde r es 0-4 y cada uno de los R2 puede ser igual o diferente, en donde (R2)2 también puede formar un anillo con C representado por cicloalquilo C3-9, alquilo bicíclico C7-12, C10-16 alquilo tricíclico C10-16, o un anillo heterocíclico mono- o bicíclico de 5- a 7 miembros que puede estar saturado o insaturado, y que contiene de uno a tres heteroátomos seleccionados entre el grupo consistente en N, O y S; fórmulas (2) y (3) donde s es 0 o 1, o R2CF2C(R12)2; R2 es fenilo, naftilo, o bifenilo, cada uno de los cuales está sin substituir o substituido con uno o más de alquilo C1-4, alcoxi C1-4, halógeno, hidroxi, CF3, OCF3, COOH, CO2R21, CONH2, CONR22R23, SO2alquilo, SO2NH2, o SO2NR22R23, un anillo heterocíclico o heteroarilo monocíclico de 5 a 7 miembros o bicíclico de 9 a 10 miembros, que puede estar saturado o insaturado, en donde el anillo heterocíclico o heteroarilo contiene de uno a cuatro heteroátomos seleccionados entre el grupo consistente en N, O y S, en donde los heteroátomos nitrógeno y azufre están opcionalmente oxidados, y en donde el anillo heterocíclico o heteroarilo están sin substituir o está substituido con uno o más de los siguientes alquilo C1-4, alcoxi C1-4, halógeno, hidroxi, CF3, OCF3, COOH, CO2R21, CONH2, CONR22R23, SO2alquilo, SO2NH2, o SO2NR22R23, cicloalquilo C3-9, que está sin substituir o está substituido con uno o más de los siguientes alquilo C1-4, alcoxi C1-4, halógeno, hidroxi, CF3, OCF3, COOH, CO2R21, CONH2, CONR22R23, SO2alquilo, SO2NH2, o SO2NR22R23, o alquilo bicíclico C7-12, que está sin substituir o está substituido con uno o más de los siguientes alquilo C1-4, alcoxi C1-4, halógeno, hidroxi, CF3, OCF3, COOH, CO2R21, CONH2, CONR22R23, SO2alquilo, SO2NH2, o SO2NR22R23; Y es -NH- ú O; R3 es hidrógeno, halógeno ú OH; R4 y R5 son independientemente hidrógeno, halógeno, alquilo, alquenilo, alquinilo, hidroxi, alcoxi, haloalquilo, haloalcoxi, hidroxialquilo, ciano, nitro, -CO2Rx,-CH2ORx o -ORx, donde Rx, en cada caso, es independientemente hidrógeno o alquilo C1-6; R6 es ciano o acetilenilo; R11 es hidrógeno, halógeno o alquilo; R12 es hidrógeno o halógeno, alquilo C1-6, no substituido o substituido con uno o más de hidroxi, COOH, amino, o halógeno, CF3; R21 es alquilo C1-8, cicloalquilo C1-8, alquil C1-8 éter, o cicloalquil C1-8 éter; R22 y R23 son, independientemente hidrógeno, alquilo C1-8, cicloalquilo C1-8, alquil C1-8 éter, o cicloalquil C1-8 éter o tomados conjuntamente con el átomo de nitrógeno al cual están enlazados, R22 y R23 forman un anillo saturado de 3 a 9 miembros, que opcionalmente tiene de 0 a 2 heteroátomos adicionales seleccionados entre nitrógeno u oxígeno; B está seleccionado a partir del el grupo consistente en las fórmulas (4), (5) y (6); en donde R7, R8, R9, y R10 son independientemente hidrógeno o alquilo; X es -O-, -NR18 -, o -CH=N- (donde N está ligado a NR13) donde R18 es hidrógeno o alquilo, estando dicho alquilo opcionalmente substituido con amino, monoalquilamino, dialquilamino, alcoxi, hidroxi, carboxi, alcoxicarbonilo, ariloxicarbonilo, aralcoxicarbonilo, acilamino, ciano o trifluorometilo; Ra, Rb y Rc son independientemente hidrógeno, alquilo, hidroxi, alcoxi, alcoxicarboniloxi, ciano o -CO2Rw; donde Rw es alquilo C1-12, cicloalquilo C3-9, arilo C6-14, ar C6-14 alquilo C1-12, o de fórmulas (7) u (8), donde Re y Rf son independientemente hidrógeno, alquilo C1-6, alquenilo C2-6 o arilo C6-14, Rg es hidrógeno, alquilo C1-6, alquenilo C2-6 o arilo C6-14, Rh es hidrógeno, alquilo C1-6, alquenilo C2-6 o arilo C6-14, y Ri es ar C6-14 alquilo C1-12 o alquilo C1-12; n es de 0 a 2; m es de 0 a 2; R13 es hidrógeno o alquilo; R14 y R15 son independientemente hidrógeno, alquilo, cicloalquilo, halógeno o alcoxi; R16 y R17 son independientemente hidrógeno, alquilo, hidroxi, alcoxi, ciano o -CO2Rj, donde Rj es alquilo C1-12, cicloalquilo C3-9, arilo C6-14, ar C6-14 alquilo C1-12, haloalquilo C1-12 o de fórmula (9), donde Re, Rf y Rg son independientemente hidrógeno o alquilo C1-12; y A es un anillo heterocíclico o heteroarilo bicíclico de 9 a 10 miembros que puede estar saturado o insaturado; en donde el anillo heterocíclico o heteroarilo contiene de 3 a 5 heteroátomos seleccionados a partir el grupo consistente en N, O y S, y está opcionalmente substituido con uno o más de los siguientes, halógeno, hidroxi, alquilo, alcoxi, o -NR19R20, donde R19 y R20 son independientemente hidrógeno o alquilo; o en donde el anillo heterocíclico o heteroarilo contiene de uno a dos heteroátomos seleccionados a partir de N, y está monosubstituido con -NR19R20, donde R19 y R20 son independientemente hidrógeno o alquilo C1-4, o en donde el anillo heterocíclico o heteroarilo contiene de uno a dos heteroátomos seleccionados a partir del grupo consistente en N, O, S, uno de los cuales debe ser O ó S, y está opcionalmente substituido con uno o más de halógeno, hidroxi, alquilo, alcoxi, o -NR19R20, donde R19 y R20 son independientemente hidrógeno o alquilo C1-4.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US46142103P | 2003-04-10 | 2003-04-10 | |
US10/816,544 US7550474B2 (en) | 2003-04-10 | 2004-04-01 | Substituted phenyl acetamides and their use as protease inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
AR044512A1 true AR044512A1 (es) | 2005-09-14 |
Family
ID=33299805
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040101198A AR044512A1 (es) | 2003-04-10 | 2004-04-07 | Fenil acetamidas sustituidas, y su utilizacion como inhibidores de las proteasas |
Country Status (8)
Country | Link |
---|---|
US (1) | US7550474B2 (es) |
EP (1) | EP1613319B1 (es) |
JP (1) | JP2006522809A (es) |
AR (1) | AR044512A1 (es) |
AT (1) | ATE432703T1 (es) |
DE (1) | DE602004021365D1 (es) |
TW (1) | TW200508200A (es) |
WO (1) | WO2004091613A2 (es) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
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SMP200700038B (it) | 2005-02-22 | 2007-09-26 | Ranbaxy Lab Ltd | Derivati dell'acido pentanoico 5-fenile come inibitori delle metalloproteinasi della matrice per il trattamento dell'asma e di altre malattie |
CN101228129A (zh) * | 2005-04-20 | 2008-07-23 | 詹森药业有限公司 | 氟代吡啶n-氧化物凝血酶调节剂和含氮杂芳基化合物的n-氧化方法 |
WO2007109459A2 (en) | 2006-03-21 | 2007-09-27 | Janssen Pharmaceutica, Nv | Pyridines and pyridine n-oxides as modulators of thrombin |
KR20110086152A (ko) | 2008-11-14 | 2011-07-27 | 다이닛본 스미토모 세이야꾸 가부시끼가이샤 | 바이페닐아세트아미드 유도체 |
JP5578705B2 (ja) * | 2010-03-29 | 2014-08-27 | 公益財団法人相模中央化学研究所 | (アリール)ジフルオロ酢酸エステル誘導体及びその製造方法 |
ES2603032T3 (es) | 2010-07-15 | 2017-02-23 | Bayer Intellectual Property Gmbh | Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas |
CN110105237B (zh) * | 2019-06-06 | 2021-12-24 | 东北师范大学 | 一种β-偕二氟叠氮化合物及其制备和应用 |
CN113292499A (zh) * | 2020-02-24 | 2021-08-24 | 齐鲁制药有限公司 | 一种β-内酰胺酶抑制剂的新制备方法及其中间体 |
CN115160134B (zh) * | 2022-08-10 | 2023-10-10 | 无锡科华生物科技有限公司 | 一种4-溴-2-甲基苯甲酸甲酯的制备方法 |
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2004
- 2004-04-01 US US10/816,544 patent/US7550474B2/en active Active
- 2004-04-01 EP EP04749611A patent/EP1613319B1/en not_active Expired - Lifetime
- 2004-04-01 JP JP2006509582A patent/JP2006522809A/ja not_active Withdrawn
- 2004-04-01 AT AT04749611T patent/ATE432703T1/de not_active IP Right Cessation
- 2004-04-01 WO PCT/US2004/010034 patent/WO2004091613A2/en active Application Filing
- 2004-04-01 DE DE602004021365T patent/DE602004021365D1/de not_active Expired - Fee Related
- 2004-04-07 AR ARP040101198A patent/AR044512A1/es not_active Application Discontinuation
- 2004-04-08 TW TW093109742A patent/TW200508200A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
ATE432703T1 (de) | 2009-06-15 |
US7550474B2 (en) | 2009-06-23 |
WO2004091613A3 (en) | 2005-01-27 |
DE602004021365D1 (de) | 2009-07-16 |
EP1613319A2 (en) | 2006-01-11 |
JP2006522809A (ja) | 2006-10-05 |
US20040254166A1 (en) | 2004-12-16 |
EP1613319B1 (en) | 2009-06-03 |
TW200508200A (en) | 2005-03-01 |
WO2004091613A2 (en) | 2004-10-28 |
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