AR058094A1 - Inhibidores nnrt basados en fenil-acetamida - Google Patents
Inhibidores nnrt basados en fenil-acetamidaInfo
- Publication number
- AR058094A1 AR058094A1 ARP060104513A ARP060104513A AR058094A1 AR 058094 A1 AR058094 A1 AR 058094A1 AR P060104513 A ARP060104513 A AR P060104513A AR P060104513 A ARP060104513 A AR P060104513A AR 058094 A1 AR058094 A1 AR 058094A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- group
- independently
- haloalkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/29—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
- C07C311/46—Y being a hydrogen or a carbon atom
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- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/56—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
- C07C311/23—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
- C07C311/24—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/31—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
- C07C311/35—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/52—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente proporciona compuestos utiles para el tratamiento de una infeccion del VIH, para prevenir una infeccion del VIH, o para tratar el SIDA o el ARC. Los compuestos de la presente son de la formula (1), en la que e R1 a R4 y Ar tienen los significados definidos anteriormente. Se describen también en la presente, métodos de tratamiento de una infeccion del VIH con compuestos definidos en esta solicitud y composiciones farmacéuticas que contienen dichos compuestos. Reivindicacion 1: Un compuesto de la formula (1) en la que: R1 es halogeno, alquilo C1-6, alcoxi C1-6, nitro o amino; R2 es H o F; R3 es fenilo sustituido de 1 a 3 veces por sustituyentes elegidos con independencia entre sí entre el grupo formado por alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, halogeno, ciano y nitro; R4 es H, alquilo C1-6 o halogeno; Ar es un anillo fenilo sustituido de la formula (2) con la condicion de que R7a y R7c no sean ambos H o que si R7c es H, entonces R7a es halogeno, haloalquilo C1-6, alcoxi C1-6, ciano o alquilo C1-6; en la que R7a se elige entre el grupo formado por H, alquilo C1-6, haloalquilo C1-3, cicloalquilo C3-7, alcoxi C1-6, haloalcoxi C1-6, halogeno y ciano; R7c se elige entre el grupo formado por halogeno, -S(O)2N-R8R9, -X2CH2(CH2)pS(O)2NR8R9; -X4(CH2)vCOOR10, -X4(CH2)vCN, -OR13, -CO2R11, -CN, -CONR8aR9a y X4(CH2)vCONR8aR9a; R7b con independencia de su aparicion se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, amino-alquilsulfonilo C1-6, SO2NR11aR11b, haloalcoxi C1-6, haloalquiltio C1-6, halogeno, hidroxi, amino, alquilamino C1-6, di(alquil C1-6)amino, aminoacilo, acilo, CONR8R9, nitro, ciano y heteroalcoxi C1-6; R8 y R9 (i) tomados independientemente, uno de R8 y R9 es H o alquilo C1-6 y el otro de R8 y R9 se elige entre el grupo formado por H, alquilo C1-6, -C(=O)R12, -(CH2)2N[(CH2)2]2X3 o -(CH2)2NR11aR11b; o (ii) R8 y R9 tomados juntos son (CH2)2-X3-(CH2)2 o -(CH2)o- opcionalmente sustituidos por 1 o 2 sustituyentes elegidos entre el grupo formado por halogeno, hidroxilo y NR11aR11b; R8a y R9a (i) tomados independientemente, uno de R8 y R9 es H o alquilo C1-6 y el otro de R8 y R9 se elige entre el grupo formado por H, hidroxialquilo C1-6, -(CH2)vN[(CH2)2]2X3 y -(CH2)vNR11aR11b o, (ii) R8a y R9a junto con el N al que están unidos son pirrolidina, piperidina; dicha pirrolidina o dicha piperidina están opcionalmente sustituidas por un hidroxilo o (iii) R8a y R9a tomados juntos son (CH2)2-X3-(CH2)2; R10 es alquilo C1-6; R11 es H o alquilo C1-6; R11a y R11b con independencia entre sí son R11; R12 es alquilo C1-10, -(CH2)sNHR11aR11b, -(CH2)sOR11, -CH2-CH(OH)CH3, - CH2N[(CH2)2]2O, -(CH2)2CO2R11, fenilo o piridinilo opcionalmente sustituidos; R13 es H o alquilo C1-6; X2 es -O- o un enlace; X3 es -O-, -S(O)n- o NR11; X4 es O-o -S(O)n-; m y n con independencia entre sí son numeros enteros de 0 a 2; o es un numero entero de 4 a 6; p es un numero entero de 0 a 6; s es un numero entero de 1 a 2; v es un numero entero de 1 a 6; y los hidratos, solvatos y las sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US72844305P | 2005-10-19 | 2005-10-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR058094A1 true AR058094A1 (es) | 2008-01-23 |
Family
ID=37606927
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060104513A AR058094A1 (es) | 2005-10-19 | 2006-10-17 | Inhibidores nnrt basados en fenil-acetamida |
Country Status (12)
Country | Link |
---|---|
US (1) | US7388111B2 (es) |
EP (1) | EP1940781A1 (es) |
JP (1) | JP2009515826A (es) |
KR (1) | KR20080056220A (es) |
CN (1) | CN101291905A (es) |
AR (1) | AR058094A1 (es) |
AU (1) | AU2006303368B2 (es) |
BR (1) | BRPI0617720A2 (es) |
CA (1) | CA2625047A1 (es) |
IL (1) | IL190442A0 (es) |
TW (1) | TW200804244A (es) |
WO (1) | WO2007045573A1 (es) |
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KR101542629B1 (ko) * | 2007-05-30 | 2015-08-06 | 에프. 호프만-라 로슈 아게 | 비-뉴클레오사이드 역전사효소 억제제 |
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BRPI0820162A2 (pt) * | 2007-11-20 | 2019-09-24 | Merck Sharp & Dohme | composto, composição farmacêutica, método para a profilazia ou tratamento de infecção pela hiv ou para a profilaxia, tratamento ou retardo no início da aids |
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BRPI0510059B8 (pt) * | 2004-04-23 | 2021-05-25 | Hoffmann La Roche | inibidores da transcriptase reversa não-nucleosídica e seus usos |
US7166738B2 (en) | 2004-04-23 | 2007-01-23 | Roche Palo Alto Llc | Non-nucleoside reverse transcriptase inhibitors |
RU2006146608A (ru) | 2004-06-09 | 2008-07-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | ОКТАГИДРОПИРРОЛО[3,4-с]-ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПРОТИВОВИРУСНЫХ АГЕНТОВ |
EP1773790B1 (en) | 2004-07-27 | 2012-08-15 | F.Hoffmann-La Roche Ag | Benzyltriazolone compounds as non-nucleoside reverse transcriptase inhibitors |
EP1831157A2 (en) | 2004-12-22 | 2007-09-12 | Pfizer Limited | Nonnucleoside inhibitors of hiv-1 reverse transcriptase |
CL2007002105A1 (es) * | 2006-07-21 | 2008-02-22 | Hoffmann La Roche | Compuestos derivados de 2-[3-(3-cianofenoxi)(fenoxi o fenilsulfanil)]-n-fenil acetamida, inhibidores de la transcriptasa inversa del vih; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar u |
-
2006
- 2006-10-09 WO PCT/EP2006/067193 patent/WO2007045573A1/en active Application Filing
- 2006-10-09 CN CNA2006800387554A patent/CN101291905A/zh active Pending
- 2006-10-09 KR KR1020087009229A patent/KR20080056220A/ko not_active Application Discontinuation
- 2006-10-09 EP EP06807082A patent/EP1940781A1/en not_active Withdrawn
- 2006-10-09 CA CA002625047A patent/CA2625047A1/en not_active Abandoned
- 2006-10-09 AU AU2006303368A patent/AU2006303368B2/en not_active Expired - Fee Related
- 2006-10-09 JP JP2008536014A patent/JP2009515826A/ja not_active Ceased
- 2006-10-09 BR BRPI0617720-4A patent/BRPI0617720A2/pt not_active IP Right Cessation
- 2006-10-16 TW TW095138066A patent/TW200804244A/zh unknown
- 2006-10-17 AR ARP060104513A patent/AR058094A1/es not_active Application Discontinuation
- 2006-10-18 US US11/583,346 patent/US7388111B2/en not_active Expired - Fee Related
-
2008
- 2008-03-26 IL IL190442A patent/IL190442A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
CN101291905A (zh) | 2008-10-22 |
US20070088053A1 (en) | 2007-04-19 |
EP1940781A1 (en) | 2008-07-09 |
BRPI0617720A2 (pt) | 2011-08-02 |
AU2006303368B2 (en) | 2011-05-26 |
AU2006303368A1 (en) | 2007-04-26 |
CA2625047A1 (en) | 2007-04-26 |
KR20080056220A (ko) | 2008-06-20 |
WO2007045573A1 (en) | 2007-04-26 |
JP2009515826A (ja) | 2009-04-16 |
IL190442A0 (en) | 2008-11-03 |
TW200804244A (en) | 2008-01-16 |
US7388111B2 (en) | 2008-06-17 |
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