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AR069832A1 - Inhibidores de la polimerasa virica - Google Patents

Inhibidores de la polimerasa virica

Info

Publication number
AR069832A1
AR069832A1 ARP080105541A ARP080105541A AR069832A1 AR 069832 A1 AR069832 A1 AR 069832A1 AR P080105541 A ARP080105541 A AR P080105541A AR P080105541 A ARP080105541 A AR P080105541A AR 069832 A1 AR069832 A1 AR 069832A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
het
aryl
independently selected
Prior art date
Application number
ARP080105541A
Other languages
English (en)
Inventor
Marc-Andre Joly
Julie Naud
Cedrickx Godbout
Martin Poirier
Jean Rancourt
Pasquale Forgione
Alexandre Gagnon
Pierre L Beaulieu
Montse Llinas-Brunet
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR069832A1 publication Critical patent/AR069832A1/es

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/63—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/38—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86—Oxygen atoms
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C07D213/643—2-Phenoxypyridines; Derivatives thereof
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
    • 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
    • C07D215/16—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 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
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    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
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    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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Abstract

Composicion farmacéutica y uso para tratar el virus de la hepatitis C (VHC). Reivindicacion 1: Un isomero, racemato, enantiomero o diastereoisomero de un compuesto de formula (1),en donde: X se selecciona de O y S; R2 es Het o arilo, opcionalmente sustituido con 1 a 5 sustituyentes R20, en donde R20, en cada caso, se selecciona independientemente de: a) halogeno, ciano o nitro; b) R7, -C(=O)R7, -C(=O)-O-R7, -O-R7, -S-R7, -SO-R7, -SO2-R7, -alquilen C1-6-R7, -alquilen C1-6-C(=O)-R7, -alquilen C1-6-C(=O)-O-R7, -alquilen C1-6-O-R7, alquilen C1-6-S-R7, alquilen C1-6-SO-R7 o alquilen C1-6-SO2-R7, en donde R7, en cada caso, se selecciona independientemente entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogenoalquilo C1-6, cicIoalquilo C3-7, cicloalquil C3-7-alquilo C1-6, arilo y Het; en donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogenoalquilo C1-6, cicIoalquilo C3-7, cicloalquil C3-7-alquilo C1-6, y alquileno C1-6 están opcionalmente sustituidos con 1 o 2 sustituyentes, cada uno independientemente seleccionado entre -OH, -alquilo C1-6 (opcionalmente sustituido con -O-alquilo C1-6), halogeno, -halogenoalquilo C1-6, cicloalquilo C3-7, -O-alquilo C1-6, ciano, COOH, -NH2, -NH-alquilo C1-4, -NH-cicloaIquilo C3-7, -N(alquiI C1-4-cicloalquilo C3-7), -N(alquilo C1-4)2, arilo, -alquiI C1-6-ariIo, Het, -alquil C1-6-Het; y en donde cada uno del arilo y Het está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno independientemente seleccionado de i) halogeno, ciano, oxo, tioxo, imino, -OH, -O-alquilo C1-6, -O-halogenoalquilo C1-6, cicloalquilo C3-7, halogenoalquilo C1-6, -C(=O)-alquilo C1-6, -SO2-alquilo C1-6, -C(=O)-NH2, -C(=O)-NH-alquilo C1-4, -C(=O)-N(alquilo C1-4)2, -C(=O)-NH-cicloalquilo C3-7, -C(=O)-N(alquil C1-4)-cicloalquilo C3-7, -NH2, -NH-alquilo C1-4, -N(alquilo C1-4)2, -NH-cicloalquilo C3-7, -N(alquil C1-4-cicloalquilo C3-7) o -NH-C(=O)-alquilo C1-4; ii) alquilo C1-6 opcionalmente sustituido con -OH, -O-halogenoalquilo C1-6 o -O-alquilo C1-6; y iii) arilo o Het, en el que cada uno del arilo y Het está opcionalmente sustituido con halogeno o alquilo C1-6; y c) -N(R8)R9, -C(=O)-N(R8)R9, -O-C(=O)-N(R8)R9, -SO2-N(R8)R9, -alquilen C1-6-N(R8)R9, -alquilen C1-6-C(=O)-N(R8)R9, -alquilen C1-6-O-C(O)N(R8)R9 o -alquilen C1-6-SO2-N(R8)R9; en donde el alquileno C1-6 está opcionalmente sustituido con 1 o 2 sustituyentes, cada uno independientemente seleccionado entre -OH, -alquilo C1-6, halogeno, -halogenoalquilo C1-6, cicloalquilo C3-7, -O-alquilo C1-6, ciano, COOH, -NH2, -NH-alquilo C1-4, -NH-cicloalquilo C3-7, -N(alquil C1-4-cicloalquiIo C3-7) y -N(alquilo C1-4)2; R8, en cada caso, se selecciona independientemente de H, alquilo C1-6 y cicloalquilo C3-7; y R9 en cada caso se selecciona independientemente de R7, -O-alquilo C1-6, -alquilen C1-6-R7, -SO2-R7, -C(=O)-R7, -C(=O)OR7 y -C(=O)N(R8)R7; en donde R7 y R8 son como se han definido antes; o R8 y R9, junto con el N al que están unidos, están unidos para formar un heterociclo de 4 a 7 miembros que además opcionalmente contiene 1 a 3 heteroátomos, cada uno independientemente seleccionado de N, O y S, en donde cada heteroátomo de S, independientemente y cuando sea posible, puede existir en un estado oxidado de modo que está además unido a uno o dos átomos de oxígeno para formar los grupos SO o SO2; en donde el heterociclo está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno independientemente seleccionado de alquilo C1-6, halogenoalquilo C1-6, halogeno, oxo, -OH, SH, -O-aIquilo C1-6, S-alquilo C1-6, cicloalquilo C3-7, -NH2, -NH-alquilo C1-6, -N(alquiloC1-6)2, -NH-cicloalquilo C3-7, -N(alquil C1-4-cicloalquilo C3-7), -C(=O)-alquilo C1-6 y -NHC(=O)-alquilo C1-6; R3, R3a y R3b se seleccionan entre H, halogeno, CN, alquilo C1-4, -OH, -O-alquilo C1-4, -S-alquilo C1-4, -NH2, -NH-alquilo C1-4, -NH-cicloalquilo C3-7, -N(alquil C1-4-cicloalquilo C3-7) y -N(alquilo C1-4)2; R5 está R51 mono-, di- o tri-sustituido con O-R52; en donde R51 es alquilo C1-6, cicloalquilo C3-7, alquil C1-6-cicloalquilo C3-7, arilo, alquiI C1-6-arilo, Het o alquil C1-6-Het, estando cada R51 opcionalmente sustituido con alquilo C1-6, cicloalquilo C3-7 o alquil C1-6-cicloalquilo C3-7; y R52 es alquilo C1-6, cicloalquilo C3-7, alquil C1-6-cicloalquilo C3-7, arilo, alquil C1-6-arilo, Het o alquil C1-6-Het, estando dichos arilo y Het opcionalmente sustituidos con alquilo C1-6 o O-alquilo C1-6; R6 es cicloaIquilo C3-7, aIquil C1-6-cicloalquilo C3-7, arilo, alquil C1-6-arilo, Het o alquil C1-6-Het; que está opcionalmente sustituido con 1 a 5 sustituyentes, cada uno independientemente seleccionado de halogeno, aIquiIo C1-6, halogenoalquilo C1-6, cicloaIquilo C3-7, -OH, -SH, -O-alquilo C1-4, -S-alquilo C1-4 y -N(R8)R9; en los que R8 y R9 son como se han definido antes; y Het es un heterociclo de 4 a 7 miembros saturado, insaturado o aromático que tiene 1 a 4 heteroátomos, cada uno independientemente seleccionado de O, N y S, o un heteropoliciclo de 7 a 14 miembros saturado, insaturado o aromático que tiene, donde sea posible, 1 a 5 heteroátomos, cada uno independientemente seleccionado de O, N y S; en el que cada heteroátomo de N, independientemente y cuando sea posible, puede existir en un estado oxidado de modo que además está unido a un átomo de oxígeno para formar un grupo N-oxido y en el que cada heteroátomo de S, independientemente y cuando sea posible, existe en un estado oxidado de modo que está además unido a uno o dos átomos de oxigeno para formar los grupos SO o SO2 o una de sus sales o ésteres. Reivindicacion 24: El compuesto de acuerdo con la reivindicacion 1 caracterizado porque tiene la formula general (2) en done R20, R3, R5 y R6 se definen como en las tablas de compuestos 1001 a 1179, sales farmacéuticamente aceptables o ésteres del mismo.
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Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7816348B2 (en) 2006-02-03 2010-10-19 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
EP2185539A4 (en) * 2007-08-03 2011-07-20 Boehringer Ingelheim Int VIRAL POLYMERASE INHIBITORS
JP2010535156A (ja) 2007-08-03 2010-11-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ウイルスポリメラーゼ阻害剤
US8476257B2 (en) 2007-12-19 2013-07-02 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US8410091B1 (en) 2009-09-11 2013-04-02 Boehringer Ingelheim International Gmbh Process for preparation of substituted 2-amino-5-(5-(heterocyclemethyl)pyridin-2-yloxy)benzoic acid
WO2012150208A1 (de) 2011-05-04 2012-11-08 Bayer Cropscience Ag Verwendung von substituierten benzylalkoholestern der cyclopropancarbonsäure zur bekämpfung von insektizid-resistenten insekten
WO2012150221A2 (de) 2011-05-04 2012-11-08 Bayer Cropscience Ag Neue halogenierte benzylalkoholester der cyclopropancarbonsäure als schädlingsbekämpfungsmittel
CN105121411B (zh) 2013-04-15 2017-10-10 杜邦公司 杀真菌酰胺
CN103601671B (zh) * 2013-10-22 2016-08-17 上海泰坦科技股份有限公司 碘代三氟甲基吡啶的制备方法
JP6905530B2 (ja) * 2015-09-16 2021-07-21 メタクリン，インク． ファルネソイドｘ受容体アゴニストとその使用
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
SG11201908330PA (en) 2017-03-15 2019-10-30 Metacrine Inc Farnesoid x receptor agonists and uses thereof
IL269068B (en) 2017-03-15 2022-09-01 Metacrine Inc Paranoid x receptor agonists and uses thereof
JP7205830B2 (ja) * 2017-08-07 2023-01-17 国立大学法人広島大学 新規アントラニル酸系化合物、並びにそれを用いたＰｉｎ１阻害剤、炎症性疾患の治療剤及び癌の治療剤
HRP20251321T1 (hr) 2018-09-18 2025-12-05 Eli Lilly And Company Agonisti farnezoid x receptora i njihova primjena
CN112739689B (zh) * 2018-12-07 2022-06-03 优迈特株式会社 含氟嘧啶化合物及其制造方法
CN111196785B (zh) * 2020-01-21 2021-08-31 成都新朝阳作物科学股份有限公司 三氮唑衍生物及其制备方法和用途
AU2021239956A1 (en) 2020-03-18 2022-10-13 Eli Lilly And Company Formulations of a farnesoid X receptor agonist
CN119504704A (zh) 2020-05-19 2025-02-25 优迈特株式会社 含氟嘧啶化合物和含氟嘧啶酮化合物

Family Cites Families (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1507457A (en) * 1974-11-12 1978-04-12 Agfa Gevaert Fixer compositions used in planographic printing
LU85544A1 (fr) * 1984-09-19 1986-04-03 Cird Derives heterocycliques aromatiques,leur procede de preparation et leur application dans les domaines therapeutique et cosmetique
GB9011833D0 (en) 1990-05-25 1990-07-18 Collins Mary K L Inhibition of viral infection
US5633388A (en) * 1996-03-29 1997-05-27 Viropharma Incorporated Compounds, compositions and methods for treatment of hepatitis C
JP2001505585A (ja) 1996-12-16 2001-04-24 藤沢薬品工業株式会社 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途
JP4452401B2 (ja) 1997-08-11 2010-04-21 ベーリンガー インゲルハイム （カナダ） リミテッド Ｃ型肝炎ウイルス阻害ペプチドアナログ
EP1003775B1 (en) 1997-08-11 2005-03-16 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptides
DE19813802A1 (de) 1998-03-27 1999-11-11 Retro Tech Gmbh Anti-virale Wirkung von Propolis durch Inhibition viraler Nukleinsäure Polymerasen
GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
CA2338490A1 (en) 1998-07-27 2000-02-10 Sergio Altamura Diketoacid-derivatives as inhibitors of polymerases
AR022061A1 (es) 1998-08-10 2002-09-04 Boehringer Ingelheim Ca Ltd Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos.
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
UA74546C2 (en) 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
JP2003528806A (ja) * 1999-07-20 2003-09-30 ダウ・アグロサイエンス・エル・エル・シー 殺菌・殺カビ性複素環式芳香族アミドおよびそれらの組成物、使用および製造方法
CN1237051C (zh) 1999-08-20 2006-01-18 道农业科学公司 杀真菌的杂环芳族酰胺和它们的组合物、使用方法和制备
WO2001047883A1 (fr) * 1999-12-27 2001-07-05 Japan Tobacco Inc. Composes a cycles accoles et leur utilisation comme medicaments
DE10012823A1 (de) * 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
US6434489B1 (en) * 2000-04-03 2002-08-13 Schering Corporation Compositions of hepatitis C virus NS5B polymerase and methods for crystallizing same
CA2405521C (en) 2000-04-05 2010-06-29 Schering Corporation Macrocyclic ns3-serine protease inhibitors of hepatitis c virus comprising n-cyclic p2 moieties
NZ521456A (en) 2000-04-19 2004-07-30 Schering Corp Macrocyclic NS3-Serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
GB0017676D0 (en) 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
AR034127A1 (es) 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
US7169760B2 (en) 2000-07-21 2007-01-30 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
ATE461207T1 (de) 2000-07-21 2010-04-15 Schering Corp Peptide als inhibitoren der ns3-serinprotease des hepatitis c virus
PE20020707A1 (es) 2000-11-20 2002-08-11 Bristol Myers Squibb Co Compuestos tripeptidicos como inhibidores de la proteasa ns3 del virus de hepatitis c
HUP0303436A2 (hu) 2000-12-12 2004-01-28 Schering Corp. Diaril-peptidek mint a hepatitis C vírus NS3-szerin proteáz inhibitorai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
IL157280A0 (en) * 2001-03-08 2004-02-19 Boehringer Ingelheim Ca Ltd Assay for identifying inhibitors of the rna dependent rna polymerase (ns5b) of hcv
EP1256628A3 (en) 2001-05-10 2003-03-19 Agouron Pharmaceuticals, Inc. Hepatitis c virus (hcv) ns5b rna polymerase and mutants thereof
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
WO2003004458A1 (en) 2001-07-03 2003-01-16 Biovitrum Ab New compounds
CA2448737C (en) * 2001-07-20 2010-06-01 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
EP2335700A1 (en) 2001-07-25 2011-06-22 Boehringer Ingelheim (Canada) Ltd. Hepatitis C virus polymerase inhibitors with a heterobicylic structure
US20030134853A1 (en) 2001-09-26 2003-07-17 Priestley Eldon Scott Compounds useful for treating hepatitis C virus
US6867185B2 (en) 2001-12-20 2005-03-15 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
GB0201179D0 (en) 2002-01-18 2002-03-06 Angeletti P Ist Richerche Bio Therapeutic agents
DE60329367D1 (de) 2002-01-23 2009-11-05 Schering Corp Verwendung bei der bekämpfung von hepatitis c virusinfektion
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
CA2370396A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
CA2369970A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
WO2003082848A1 (en) * 2002-04-01 2003-10-09 Pfizer Inc. Pyranon and pyrandion inhibitors of hepatitis c virus rna-dependent rna polymerase
PL215228B1 (pl) 2002-05-20 2013-11-29 Bristol Myers Squibb Co Zwiazki tripeptydowe, ich zastosowanie i kompozycja farmaceutyczna je zawierajaca oraz jej zastosowanie
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
DE60334205D1 (en) 2002-05-20 2010-10-28 Bristol Myers Squibb Co Heterocyclische sulfonamid-hepatitis-c-virus-hemmer
DE60324552D1 (en) 2002-05-20 2008-12-18 Bristol Myers Squibb Co Substituierte cycloalkyl p1' hepatitis c virus inhibitoren
EP1511751B1 (en) * 2002-06-04 2008-03-19 Neogenesis Pharmaceuticals, Inc. Pyrazolo[1,5-a]pyrimidine compounds as antiviral agents
CA2490666A1 (en) * 2002-07-16 2004-01-22 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
US20040138109A1 (en) 2002-09-30 2004-07-15 Boehringer Ingelheim Pharmaceuticals, Inc. Potent inhibitor of HCV serine protease
AU2003269317B2 (en) * 2002-10-23 2009-10-29 Glenmark Pharmaceuticals Ltd. Novel tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
US20050159345A1 (en) 2002-10-29 2005-07-21 Boehringer Ingelheim International Gmbh Composition for the treatment of infection by Flaviviridae viruses
WO2004041818A1 (en) 2002-11-01 2004-05-21 Abbott Laboratories Anti-infective agents
US7902203B2 (en) 2002-11-01 2011-03-08 Abbott Laboratories, Inc. Anti-infective agents
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US7098231B2 (en) * 2003-01-22 2006-08-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
CN1771050A (zh) 2003-02-07 2006-05-10 益安药业 丙型肝炎丝氨酸蛋白酶的大环抑制剂
WO2004101605A1 (en) 2003-03-05 2004-11-25 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
EP1599496B1 (en) 2003-03-05 2010-11-03 Boehringer Ingelheim International GmbH Hepatitis c inhibitor peptide analogs
JP4245377B2 (ja) 2003-03-07 2009-03-25 株式会社Ａｄｅｋａ 高弾性エポキシ樹脂組成物
GB0307891D0 (en) 2003-04-04 2003-05-14 Angeletti P Ist Richerche Bio Chemical compounds,compositions and uses
ATE422895T1 (de) 2003-04-16 2009-03-15 Bristol Myers Squibb Co Makrocyclische isochinolinpeptidinhibitoren des hepatitis-c-virus
EP2143727B1 (en) 2003-04-18 2015-01-21 Enanta Pharmaceuticals, Inc. Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors
ES2456702T3 (es) 2003-05-09 2014-04-23 Boehringer Ingelheim International Gmbh Bolsillo de unión del inhibidor de la polimerasa NS5B del virus de la hepatitis C
EA009295B1 (ru) 2003-05-21 2007-12-28 Бёрингер Ингельхайм Интернациональ Гмбх Соединения в качестве ингибиторов вируса гепатита с
WO2004113365A2 (en) 2003-06-05 2004-12-29 Enanta Pharmaceuticals, Inc. Hepatitis c serine protease tri-peptide inhibitors
GB0313250D0 (en) 2003-06-09 2003-07-16 Angeletti P Ist Richerche Bio Therapeutic agents
US7125845B2 (en) 2003-07-03 2006-10-24 Enanta Pharmaceuticals, Inc. Aza-peptide macrocyclic hepatitis C serine protease inhibitors
EP1651631A1 (en) 2003-08-01 2006-05-03 Genelabs Technologies, Inc. Bicyclic imidazol derivatives against flaviviridae
WO2005014543A1 (ja) 2003-08-06 2005-02-17 Japan Tobacco Inc. 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用
US7378414B2 (en) 2003-08-25 2008-05-27 Abbott Laboratories Anti-infective agents
WO2005019191A2 (en) 2003-08-25 2005-03-03 Abbott Laboratories 1, 1-dioxido-4h-1,2,4-benzothiadiazine derivate und verwandte verbindungen als inhibitoren der hcv polymerase zur behandlung von hepatitis c
EP1664090A2 (en) 2003-08-26 2006-06-07 Schering Corporation Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus
CA2537114C (en) 2003-08-27 2012-10-02 Biota, Inc. Tricyclic nucleosides or nucleotides as therapeutic agents
GB0321003D0 (en) 2003-09-09 2003-10-08 Angeletti P Ist Richerche Bio Compounds, compositions and uses
US7112601B2 (en) 2003-09-11 2006-09-26 Bristol-Myers Squibb Company Cycloalkyl heterocycles for treating hepatitis C virus
RS20060197A (sr) 2003-09-22 2008-09-29 Boehringer Ingelheim International Gmbh., Makrociklični peptidi koji su aktivni protiv hepatitisa c virusa
BRPI0414814A (pt) 2003-09-26 2006-11-14 Schering Corp inibidores macrocìclicos de protease de serina ns3 de vìrus de hepatite c
GB0323845D0 (en) 2003-10-10 2003-11-12 Angeletti P Ist Richerche Bio Chemical compounds,compositions and uses
RS20110578A3 (en) 2003-10-14 2016-02-29 F. Hoffmann-La Roche Ltd MACROCYCLIC CARBOXYLIC ACIDS AND ACYLSULPHONAMIDES AS HCV REPLICATION INHIBITORS
US20050119318A1 (en) 2003-10-31 2005-06-02 Hudyma Thomas W. Inhibitors of HCV replication
US7132504B2 (en) 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JPWO2005049622A1 (ja) 2003-11-19 2007-06-07 日本たばこ産業株式会社 ５−５員縮合複素環化合物及びそのｈｃｖポリメラーゼ阻害剤としての用途
CN1902216A (zh) 2003-11-20 2007-01-24 先灵公司 丙肝病毒ns3蛋白酶的去肽化抑制剂
US7309708B2 (en) 2003-11-20 2007-12-18 Birstol-Myers Squibb Company Hepatitis C virus inhibitors
US7135462B2 (en) 2003-11-20 2006-11-14 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CA2549167A1 (en) 2003-12-11 2005-06-30 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
JP4682155B2 (ja) 2004-01-21 2011-05-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃ型肝炎ウイルスに対して活性な大環状ペプチド
CN103319464A (zh) 2004-02-20 2013-09-25 贝林格尔.英格海姆国际有限公司 病毒聚合酶抑制剂
ATE428714T1 (de) 2004-02-24 2009-05-15 Japan Tobacco Inc Kondensierte heterotetracyclische verbindungen und deren verwendung als hcv-polymerase-inhibitor
WO2005087721A2 (en) 2004-02-27 2005-09-22 Schering Corporation Compounds as inhibitors of hepatitis c virus ns3 serine protease
CA2557307A1 (en) 2004-02-27 2005-09-22 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease
EP1730165A1 (en) 2004-02-27 2006-12-13 Schering Corporation Inhibitors of hepatitis c virus ns3 protease
JP2007525511A (ja) 2004-02-27 2007-09-06 シェーリング　コーポレイション Ｃ型肝炎ウイルスｎｓ３セリンプロテアーゼの新規のインヒビターとしての化合物
CN1946690A (zh) 2004-02-27 2007-04-11 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的含环丁烯二酮基团化合物
CN103102389A (zh) 2004-02-27 2013-05-15 默沙东公司 作为丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的硫化合物
JP4874227B2 (ja) 2004-02-27 2012-02-15 シェーリング コーポレイション Ｃ型肝炎ウイルスのｎｓ３セリンプロテアーゼインヒビターとしての環状ｐ４’ｓを有する新規ケトアミド
US7371743B2 (en) * 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
AR049635A1 (es) 2004-05-06 2006-08-23 Schering Corp (1r,2s,5s)-n-((1s)-3-amino-1-(ciclobutilmetil)-2,3-dioxopropil)-3-((2s)-2-((((1,1-dimetiletil)amino)carbonil)amino)-3,3-dimetil-1-oxobutil)-6,6-dimetil-3-azabiciclo(3.1.0)hexan-2-carboxamida como inhibidor de la ns3/ns4a serina proteasa del virus de la hepatitis c
EP1773868B1 (en) 2004-05-20 2009-07-15 Schering Corporation Substituted prolines as inhibitors of hepatitis c virus ns3 serine protease
GB0413087D0 (en) 2004-06-11 2004-07-14 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2005121132A1 (ja) 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗ｈｃｖ作用を有する縮合ヘテロ環化合物
EP1763531A4 (en) 2004-06-28 2009-07-01 Boehringer Ingelheim Int ANALOGUE OF HEPATITIS-C INHIBITING PEPTIDES
US20060004197A1 (en) * 2004-07-02 2006-01-05 Thomas Thrash Sulfonamide-based compounds as protein tyrosine kinase inhibitors
UY29017A1 (es) 2004-07-16 2006-02-24 Boehringer Ingelheim Int Inhibidores de polimerasa viral
ATE512971T1 (de) 2004-07-20 2011-07-15 Boehringer Ingelheim Int Peptidanaloga als hepatitis c-hemmer
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
GB0416396D0 (en) 2004-07-22 2004-08-25 Angeletti P Ist Richerche Bio Therapeutic agents
US20060025480A1 (en) * 2004-08-02 2006-02-02 Boehringer Ingelheim International Gmbh Benzoic acid derivatives as non nucleoside reverse transcriptase inhibitors
US7153848B2 (en) 2004-08-09 2006-12-26 Bristol-Myers Squibb Company Inhibitors of HCV replication
GB0419850D0 (en) 2004-09-07 2004-10-13 Angeletti P Ist Richerche Bio Therapeutic agents
US20070249637A1 (en) 2004-10-21 2007-10-25 Collins Michael R Inhibitors Of Hepatitis C Virus Protease, And Compositions And Treatments Using The Same
WO2006046039A2 (en) 2004-10-26 2006-05-04 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Tetracyclic indole derivatives as antiviral agents
CN101094847B (zh) 2004-11-02 2011-06-15 Msdk.K.公司 芳氧基取代的苯并咪唑衍生物
US7659263B2 (en) 2004-11-12 2010-02-09 Japan Tobacco Inc. Thienopyrrole compound and use thereof as HCV polymerase inhibitor
WO2006093801A1 (en) 2005-02-25 2006-09-08 Abbott Laboratories Thiadiazine derivatives useful as anti-infective agents
WO2006094347A1 (en) 2005-03-08 2006-09-14 Biota Scientific Management Pty Ltd. Bicyclic nucleosides and nucleotides as therapeutic agents
JP4705164B2 (ja) 2005-05-02 2011-06-22 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｃｖｎｓ３プロテアーゼ阻害剤
GB0509326D0 (en) 2005-05-09 2005-06-15 Angeletti P Ist Richerche Bio Therapeutic compounds
BRPI0610283A2 (pt) 2005-05-13 2010-10-19 Virochem Pharma Inc composto, uso do mesmo na preparação de um medicamento para o tratamento ou prevenção de uma infecção por vìrus de hepatite c, composição farmacêutica e combinação farmacêutica
TWI387603B (zh) 2005-07-20 2013-03-01 Merck Sharp & Dohme Ｈｃｖ ｎｓ３蛋白酶抑制劑
JP2009501732A (ja) 2005-07-20 2009-01-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃ型肝炎インヒビターペプチド類似体
AU2006274861B2 (en) 2005-07-29 2012-11-08 Medivir Ab Macrocyclic inhibitors of hepatitis C virus
JP4705984B2 (ja) 2005-08-01 2011-06-22 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｃｖｎｓ３プロテアーゼ阻害剤としての大環状ペプチド
EP1915378A4 (en) 2005-08-12 2009-07-22 Boehringer Ingelheim Int VIRUS POLYMERASE INHIBITORS
WO2007028789A1 (en) 2005-09-07 2007-03-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Quinazoline derivatives as antiviral agents
GB0518390D0 (en) 2005-09-09 2005-10-19 Angeletti P Ist Richerche Bio Therapeutic compounds
US7399758B2 (en) 2005-09-12 2008-07-15 Meanwell Nicholas A Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
US7473688B2 (en) 2005-09-13 2009-01-06 Bristol-Myers Squibb Company Indolobenzazepine HCV NS5B inhibitors
CN101267825B (zh) 2005-09-19 2011-12-28 阿罗治疗有限公司 治疗丙型肝炎感染的苯并二氮杂*衍生物
WO2007039146A1 (en) 2005-09-23 2007-04-12 Smithkline Beecham Corporation 4-carboxy pyrazole derivatives as anti-viral agents
GB0522881D0 (en) 2005-11-10 2005-12-21 Angeletti P Ist Richerche Bio Therapeutic compounds
ITRM20050611A1 (it) 2005-12-06 2007-06-07 Angeletti P Ist Richerche Bio Derivati azanucleosidici ad attivita' antivirale.
US7816348B2 (en) * 2006-02-03 2010-10-19 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
WO2007092000A1 (en) 2006-02-06 2007-08-16 Bristol-Myers Squibb Company Inhibitors of hcv replication
US7456165B2 (en) 2006-02-08 2008-11-25 Bristol-Myers Squibb Company HCV NS5B inhibitors
CA2637879A1 (en) 2006-02-14 2007-08-23 Merck & Co., Inc. Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection
GB0608928D0 (en) 2006-05-08 2006-06-14 Angeletti P Ist Richerche Bio Therapeutic agents
US7456166B2 (en) 2006-05-17 2008-11-25 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
US7521442B2 (en) 2006-05-25 2009-04-21 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
DE602007006796D1 (de) 2006-05-25 2010-07-08 Bristol Myers Squibb Co Cyclopropyl-fusionierte indolbenzazepin-hcv-ns5b-hemmer
US7452876B2 (en) 2006-06-08 2008-11-18 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
KR20090042973A (ko) * 2006-08-17 2009-05-04 베링거 인겔하임 인터내셔날 게엠베하 바이러스 폴리머라제 억제제
EP2178886A1 (en) 2007-07-17 2010-04-28 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Macrocyclic indole derivatives for the treatment of hepatitis c infections
JP2010535156A (ja) 2007-08-03 2010-11-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ウイルスポリメラーゼ阻害剤
EP2185539A4 (en) * 2007-08-03 2011-07-20 Boehringer Ingelheim Int VIRAL POLYMERASE INHIBITORS
US7442830B1 (en) * 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
JP5421925B2 (ja) 2007-12-19 2014-02-19 ジェネンテック， インコーポレイテッド ５−アニリノイミダゾピリジン及び使用の方法
TWI431010B (zh) 2007-12-19 2014-03-21 Lilly Co Eli 礦皮質素受體拮抗劑及使用方法
WO2009077497A2 (de) 2007-12-19 2009-06-25 Basf Se Azolylmethyloxirane, ihre verwendung sowie sie enthaltende mittel
TWI432421B (zh) 2007-12-19 2014-04-01 Du Pont 製備２－胺基－５－氰基苯甲酸衍生物之方法
JP2011506551A (ja) 2007-12-19 2011-03-03 グラクソ グループ リミテッド Ａｍｐａ受容体増強化合物および医薬におけるその使用
US8476257B2 (en) * 2007-12-19 2013-07-02 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
KR20100093127A (ko) 2007-12-19 2010-08-24 바스프 에스이 아졸릴메틸옥시란, 이의 용도 및 이를 포함하는 작용제
JP2011506543A (ja) 2007-12-19 2011-03-03 ビーエーエスエフ ソシエタス・ヨーロピア アゾリルメチルオキシラン、その使用及びそれを含む薬剤
US20100311581A1 (en) * 2007-12-19 2010-12-09 Basf Se Azolylmethyloxiranes, use Thereof and Agents Containing the Same
WO2009077608A1 (en) 2007-12-19 2009-06-25 Palau Pharma, S. A. 2 -aminopyrimidine derivatives as histamine h4 antagonists
US7820665B2 (en) 2007-12-19 2010-10-26 Amgen Inc. Imidazopyridazine inhibitors of PI3 kinase for cancer treatment
EP2350039A4 (en) 2008-10-03 2012-10-10 Boehringer Ingelheim Int INHIBITORS OF VIRAL POLYMERASE

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