AR044990A1 - Antibioticos de oxazolidinona sustituidos con un grupo ciclopropilo y derivados de los mismos - Google Patents
Antibioticos de oxazolidinona sustituidos con un grupo ciclopropilo y derivados de los mismosInfo
- Publication number
- AR044990A1 AR044990A1 ARP040102330A ARP040102330A AR044990A1 AR 044990 A1 AR044990 A1 AR 044990A1 AR P040102330 A ARP040102330 A AR P040102330A AR P040102330 A ARP040102330 A AR P040102330A AR 044990 A1 AR044990 A1 AR 044990A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- groups
- alkoxy
- halogen
- Prior art date
Links
Classifications
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- 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
- C07D413/10—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 carbon chain containing aromatic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Abstract
Reivindicación 1: La presente se relaciona con los compuestos de la fórmula (1), su enantiómero, diastereómero, o sal farmacéuticamente aceptable, hidrato o prodroga de los mismos caracterizados porque: R1 representa: i) hidrógeno, ii) (CH2)nNR5R6, iii) CR7R8R9, C(R)2OR14, CH2NHR14, iv) C(=O)R13, C(=NOH)H, C(=NOR13)H, C(=NOR13)R13, C(=NOH)R13, C(=O)N(R13)2; C(=NOH)N(R13)2, NHC(=X1)N(R13)2, NRCO2R, (C=NH)R7, N(R13)C(=X1)N(R13)2, COOR13, SO2R14, N(R13)SO2R14, N(R13)COR14, v) (C1-6 alquilo)CN, CN, CH=C(R)2, (CH2)pOH, C(=O)CHR13, C(=NR13)R13, NR10C(=X1)R13; o vi) C5-10 heterociclo opcionalmente sustituido con 1-3 grupos de R7, que pueden estar unidos ya sea por un carbono o por un heteroátomo; X representa una fórmula (2); o a C5-10 heteroarilo representado por el anillo N que representa un grupo heterocíclico aromático sustituido opcionalmente que contiene de 1 a 4 átomos de nitrógeno y al menos un doble enlace y que está conectado a través de un enlace en cualquier nitrógeno, heteroarilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados de R7; Y representa NR*, O, CN, o S(O)p; el anillo "a" y el anillo "b", representa arilo o heteroarilo, o heterociclo, heterociclilo o heterocíclico; R3 representa NR(C=X2)R12, NR*R12, C6-10 arilo, o -(O)nC5-10 heterocicliol que puede estar unidos a través de un carbono o un heteroátomo; dichos arilo y heterocicliol opcionalmente sustituidos con 1-3 grupos de R7; R4, R4a, R4b, y R4c independientemente representan i) hidrógeno, ii) halógeno, iii) C1-6 alcoxi, o iv) C1-6 alquilo; r y s son independientemente 1-3, con la provisión de cuando (R4a)s y (R4)r o (R4b) y (R4c)s son unidos a un anillo "a" y el anillo "b" la suma de r y s es menor o igual a 4; R5 y R6 independientemente representan: i) hidrógeno; ii) C1-6 alquilo opcionalmente sustituido con 1-3 grupos de halógeno, CN, OH, C1-6 alcoxi, amino, imino, hidroxiamino, alcoxiamino, C1-6 aciloxi, C1-6 alquilosulfenil, C1-6 alquilosulfinil, C1-6 alquilosulfonil, aminosulfonil, C1-6 alquiloaminosulfonil, C1-6 dialquiloaminosulfonil, 4-morfolinilsulfonil, fenil, piridina, 5-isoxazolil, etileniloxi, o etinil, dichos fenil y piridina opcionalmente sustituido con 1-3 halógeno, CN, OH, CF3, C1-6 alquilo o C1-6 alcoxi; iii) C1-6 acilo opcionalmente sustituido con 1-3 grupos de halógeno, OH, SH, C1-6 alcoxi, naftalenoxi, fenoxi, amino, C1-6 acilamino, hidroxilamino, alcoxilamino C1-6 aciloxi, aralquiloxi, fenil, piridina, C1-6 alquilocarbonil, C1-6 alquiloamino, C1-6 dialquiloamino, C1-6 hidroxiaciloxi, C1-6 alquilosulfenilo, ftalimido, maleimido, succinimido, dichos fenoxi, fenil y piridina opcionalmente sustituidos con grupos 1-3 de halo, OH, CN, C1-6 alcoxi, amino, C1-6 acilamino, CF3 o C1-6 alquilo; iv) C1-6 alquilosulfonil opcionalmente sustituido con 1-3 grupos de halógeno, OH, C1-6 alcoxi, amino, hidroxilamino, alcoxilamino, C1-6 aciloxi, o fenilo; dicho fenilo opcionalmente sustituido con grupos 1-3 de halo, OH, C1-6 alcoxi, amino, C1-6 acilamino, CF3 o C1-6 alquilo; v) arilosulfonil opcionalmente sustituido con 1-3 grupos de halógeno, C1-6 alcoxi, OH o C1-6 alquilo; vi) C1-6 alcoxicarbonil opcionalmente sustituido con 1-3 de halógeno, OH, C1-6 alcoxi, C1-6 aciloxi, o fenilo, dicho fenilo opcionalmente sustituido con grupos 1-3 de halo, OH, C1-6 alcoxi, amino, C1-6 acilamino, CF3 o C1-6 alquilo; vii) aminocarbonil, C1-6 alquiloaminocarbonil o C1-6 dialquiloaminocarbonil, dichos grupos alquilo opcionalmente sustituidos con grupos 1-3 de halógeno, OH, C1-6 alcoxi o fenilo; viii) cinco a seis heterociclos membrados opcionalmente sustituidos con 1-3 grupos de halógeno, OH, CN, amino, C1-6 acilamino, C1-6 alquilosulfonilamino, C1-6 alcoxicarbonilamino, C1-6 alcoxi, C1-6 aciloxi o C1-6 alquilo, dicho alquilo opcionalmente sustituido con grupos 1-3 de halógeno, o C1-6 alcoxi; ix) C3-6 cicloalquilocarbonil opcionalmente sustituido con grupos 1-3 de halógeno, OH, C1-6 alcoxi o CN; x) benzoil opcionalmente sustituido con grupos 1-3 de halógeno, OH, C1-6 alcoxi, C1-6 alquilo, CF3, C1-6 alcanoil, amino o C1-6 acilamino; xi) pirrolilcarbonil opcionalmente sustituido con 1-3 de C1-6 alquilo; xii) C1-2 aciloxiacetil donde el acil es opcionalmente sustituido con amino, C1-6 alquiloamino, C1-6 dialquiloamino, 4-morfolino, 4-aminofenil, 4-(dialquiloamino)fenil, 4-(glicilamino)fenil; o R5 y R6 tomados junto con cualquier átomo pueden formar un anillo heterocíclico de 7 miembros que contiene átomos de carbono y 1-2 heteroátomos independientemente elegidos de O, S, SO, SO2, N, o NR8; R7 i) hidrógeno, halógeno, (Ch2)pC5-10 heterocicliol, CN, CO2R, CON(R)2, CHO, (CH2)0-3NHAc, C(=NOR), OH, C1-6 alcoxi, C1-6 alquilo, alquenilo, hidroxi C1-6 alquilo, (CH2)1-3NHC(O)C1-6 alquilo, (CH2)0-3N(C1-6 alquilo)2, NHCO2R, -OCOC1-6 alquilo; ii) (CH2)namino, (CH2)nC1-6 alquiloamino, C1-6 acilamino, C1-6 dialquiloamino, hidroxilamino o C1-2 alcoxiamino los cuales pueden todos ser opcionalmente sustituidos en el nitrógeno con c1-6 acil, C1-6 alquilosulfonil o C1-6 alcoxicarbonil, dicho acil y alquilosulfonil opcionalmente sustituidos con 1-2 de halógeno o OH; R8 y R9 independientemente representa i) H, CN, ii) C1-6 alquilo opcionalmente sustituido con 1-3 halógeno, CN, OH, C1-6 alcoxi, C1-6 aciloxi, o amino, iii) fenilo opcionalmente sustituido con 1-3 grupos de halógeno, OH, C1-6 alcoxi; o R7 y R8 tomados juntos pueden formar un anillo de carbono de 3-7 miembros opcionalmente interrumpido con 1-2 heteroátomos elegidos de O, S, SO, SO2, NH, y NR8; X1 representa O, S o NR13, NCN, NCO2R16, o NSO2R14; X2 representa O, S, NH o NSO2R14; R10 representa hidrógeno, C1-6 alquilo o CO2R15; R12 representa hidrógeno, C1-6 alquilo, NH2, OR, CHF2, CHCl2, C(R)2Cl, (CH2)nSR, (CH2)nCN, (CH2)nSO2R, (CH2)nS(O)R, C1-6 alquiloamino, C3-6 cicloalquilo, C5-10 heterocicliol o C1-6 dialquiloamino, donde dichos alquilo, y cicloalquilo pueden ser sustituidos con 1-3 grupos de halo, CN, OH o C1-6 alcoxi, dicho heterocicliol opcionalmente sustituido con 1-3 grupos de R7; cada R13 representa independientemente hidrógeno, C1-6 alquilo, C6-10 arilo, NR5R6, SR8, S(O)R8, S(O)2R8, CN, OH, C1-6 alquiloS(O)R, C1-6 alcoxicarbonil, hidroxicarbonil, -OCOarilo, C1-6 acil, C3-7 anillo de carbono membrado opcionalmente interrumpido con 1-4 heteroátomos elegidos de O, S, SO, SO2, NH y NR8 donde dichos grupos C1-6 alquilo, arilo o C1-6 acil pueden ser independientemente sustituidos con 0-3 grupos halógenos, hidroxi, N(R)2, CO2R, C6-10 arilo, C5-10 heteroarilo, o C1-6 alcoxi; cuando dos grupos R13 se unen al mismo átomo o a dos átomos adyacentes pueden estar juntos para formar un anillo de carbono de 3-7 miembros opcionalmente interrumpido con 1-2 heteroátomos elegidos de O, S, SO, SO2, NH, y NR8; R representa hidrógeno o C1-6 alquilo; R* representa hidrógeno, CN, C(=O)R14, (CH2)pCO2C1-6 alquilo, (CH2)pC5-10 heterocicliol, o C1-6 alquilo, dicho alquilo y heterocicliol opcionalmente sustituidos con 1 a 3 grupos de R7; R14 representa amino, C1-6 alquilo, C3-6 cicloalquilo, (CH2)pC5-10 heterocicliol, C1-6 haloalquilo, fenilo, dicho alquilo, cicloalquilo, fenilo, heterocicliol opcionalmente sustituidos con 1-3 grupos de R7, cuando R7 es un amino o grupo hidroxilo o un nitrógeno que forma parte del heterociclo, dicho amino y hidroxi opcionalmente protegidos con un amino o un grupo protector hidroxi; R15 es C1-6 alquilo o bencilo dicho bencilo opcionalmente sustituido con 1-3 grupos de halo, OH, C1-6 alcoxi, amino, C1-6 acilamino, o C1-6 alquilo; R16 es hidrógeno, C5-10 heteroarilo, C6-10 arilo, dichos heteroarilo y arilo opcionalmente sustituidos con 1-3 grupos de R7; p representa 0-2 y n representa 0-1.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US48390403P | 2003-07-02 | 2003-07-02 | |
US54698404P | 2004-02-24 | 2004-02-24 |
Publications (1)
Publication Number | Publication Date |
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AR044990A1 true AR044990A1 (es) | 2005-10-12 |
Family
ID=34068173
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040102330A AR044990A1 (es) | 2003-07-02 | 2004-07-01 | Antibioticos de oxazolidinona sustituidos con un grupo ciclopropilo y derivados de los mismos |
Country Status (23)
Country | Link |
---|---|
US (2) | US7462633B2 (es) |
EP (1) | EP1646629B1 (es) |
JP (1) | JP4607107B2 (es) |
KR (1) | KR20060113625A (es) |
AR (1) | AR044990A1 (es) |
AT (1) | ATE471937T1 (es) |
AU (1) | AU2004256083B2 (es) |
BR (1) | BRPI0411688A (es) |
CA (1) | CA2530140C (es) |
CL (1) | CL2004001678A1 (es) |
DE (1) | DE602004027811D1 (es) |
EC (1) | ECSP056257A (es) |
IL (1) | IL172785A0 (es) |
IS (1) | IS8178A (es) |
MA (1) | MA27938A1 (es) |
MX (1) | MXPA06000228A (es) |
MY (1) | MY140137A (es) |
NO (1) | NO20060558L (es) |
NZ (1) | NZ544237A (es) |
PE (1) | PE20050732A1 (es) |
RU (1) | RU2348628C2 (es) |
TW (1) | TW200510421A (es) |
WO (1) | WO2005005398A2 (es) |
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US8324398B2 (en) * | 2003-06-03 | 2012-12-04 | Rib-X Pharmaceuticals, Inc. | Process for the synthesis of biaryl oxazolidinones |
PL1656370T3 (pl) * | 2003-06-03 | 2013-03-29 | Melinta Subsidiary Corp | Biarylowe związki heterocykliczne oraz sposoby ich wytwarzania i stosowania |
EP1646630A1 (en) * | 2003-07-02 | 2006-04-19 | Merck & Co., Inc. | Oxazolidinone antibiotics and derivatives thereof |
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EP1713785A1 (en) * | 2003-12-17 | 2006-10-25 | Rib-X Pharmaceuticals, Inc. | Halogenated biaryl heterocyclic compounds and methods of making and using the same |
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TW200500360A (en) | 2003-03-01 | 2005-01-01 | Astrazeneca Ab | Hydroxymethyl compounds |
EP1615916A1 (en) | 2003-04-09 | 2006-01-18 | Pharmacia & Upjohn Company LLC | Antimicrobial 3.1.0 bicyclohexylphenyl-oxazolidinone derivatives and analogues |
AU2003223034A1 (en) | 2003-05-06 | 2004-11-26 | Ranbaxy Laboratories Limited | Oxazolidinone derivatives as antimicrobials |
EP1646630A1 (en) | 2003-07-02 | 2006-04-19 | Merck & Co., Inc. | Oxazolidinone antibiotics and derivatives thereof |
JP2007521283A (ja) | 2003-07-02 | 2007-08-02 | メルク アンド カンパニー インコーポレーテッド | シクロプロピル基で置換されたオキサゾリジノン系抗生物質およびその誘導体 |
RU2348628C2 (ru) * | 2003-07-02 | 2009-03-10 | Мерк Энд Ко., Инк. | Замещенные циклопропильной группой оксазолидиноновые антибиотики и их производные |
AU2004256084B2 (en) | 2003-07-02 | 2007-10-18 | Kyorin Pharmaceutical Co., Ltd. | Oxazolidinone antibiotics and derivatives thereof |
-
2004
- 2004-06-29 RU RU2005140379/04A patent/RU2348628C2/ru not_active IP Right Cessation
- 2004-06-29 BR BRPI0411688-7A patent/BRPI0411688A/pt not_active IP Right Cessation
- 2004-06-29 MX MXPA06000228A patent/MXPA06000228A/es active IP Right Grant
- 2004-06-29 US US10/878,637 patent/US7462633B2/en not_active Expired - Fee Related
- 2004-06-29 JP JP2006517736A patent/JP4607107B2/ja not_active Expired - Fee Related
- 2004-06-29 CA CA2530140A patent/CA2530140C/en not_active Expired - Fee Related
- 2004-06-29 AT AT04777196T patent/ATE471937T1/de not_active IP Right Cessation
- 2004-06-29 KR KR1020067000071A patent/KR20060113625A/ko not_active Application Discontinuation
- 2004-06-29 AU AU2004256083A patent/AU2004256083B2/en not_active Ceased
- 2004-06-29 WO PCT/US2004/020734 patent/WO2005005398A2/en active Search and Examination
- 2004-06-29 EP EP04777196A patent/EP1646629B1/en active Active
- 2004-06-29 NZ NZ544237A patent/NZ544237A/en unknown
- 2004-06-29 DE DE602004027811T patent/DE602004027811D1/de active Active
- 2004-07-01 AR ARP040102330A patent/AR044990A1/es unknown
- 2004-07-01 MY MYPI20042639A patent/MY140137A/en unknown
- 2004-07-01 CL CL200401678A patent/CL2004001678A1/es unknown
- 2004-07-01 PE PE2004000629A patent/PE20050732A1/es not_active Application Discontinuation
- 2004-07-02 TW TW093120081A patent/TW200510421A/zh unknown
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2005
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- 2005-12-22 IL IL172785A patent/IL172785A0/en unknown
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2006
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- 2006-02-02 NO NO20060558A patent/NO20060558L/no not_active Application Discontinuation
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AU2004256083B2 (en) | 2007-10-11 |
ECSP056257A (es) | 2006-04-19 |
CA2530140C (en) | 2010-11-09 |
JP4607107B2 (ja) | 2011-01-05 |
US7462633B2 (en) | 2008-12-09 |
CA2530140A1 (en) | 2005-01-20 |
MA27938A1 (fr) | 2006-06-01 |
AU2004256083A1 (en) | 2005-01-20 |
KR20060113625A (ko) | 2006-11-02 |
EP1646629B1 (en) | 2010-06-23 |
MXPA06000228A (es) | 2006-06-27 |
US20050038092A1 (en) | 2005-02-17 |
IL172785A0 (en) | 2006-06-11 |
ATE471937T1 (de) | 2010-07-15 |
RU2348628C2 (ru) | 2009-03-10 |
US20070203187A1 (en) | 2007-08-30 |
NZ544237A (en) | 2008-09-26 |
NO20060558L (no) | 2006-02-02 |
IS8178A (is) | 2005-12-13 |
WO2005005398A3 (en) | 2005-04-28 |
EP1646629A2 (en) | 2006-04-19 |
WO2005005398A2 (en) | 2005-01-20 |
US7582659B2 (en) | 2009-09-01 |
JP2007521281A (ja) | 2007-08-02 |
TW200510421A (en) | 2005-03-16 |
RU2005140379A (ru) | 2007-08-10 |
BRPI0411688A (pt) | 2006-12-26 |
PE20050732A1 (es) | 2005-11-02 |
DE602004027811D1 (de) | 2010-08-05 |
CL2004001678A1 (es) | 2005-05-20 |
MY140137A (en) | 2009-11-30 |
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