AR045596A1 - Inhibidores de proteasas de serina en particular proteasa ns3-ns4a del vhc - Google Patents

Inhibidores de proteasas de serina en particular proteasa ns3-ns4a del vhc

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Publication number
AR045596A1
AR045596A1 ARP040103191A ARP040103191A AR045596A1 AR 045596 A1 AR045596 A1 AR 045596A1 AR P040103191 A ARP040103191 A AR P040103191A AR P040103191 A ARP040103191 A AR P040103191A AR 045596 A1 AR045596 A1 AR 045596A1
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AR
Argentina
Prior art keywords
aliphatic
heteroaryl
cycloalkyl
aryl
independently
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Application number
ARP040103191A
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English (en)
Inventor
Robert B Perni
John J Court
Shawn D Britt
Janos Pitlik
Drie John H Van
Original Assignee
Vertex Pharma
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Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR045596A1 publication Critical patent/AR045596A1/es

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    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
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    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/60—1,4-Diazines; Hydrogenated 1,4-diazines
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • 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
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    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • 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
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    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
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    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D401/02—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 containing two hetero rings
    • C07D401/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—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 containing three or more hetero rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
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    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Abstract

Compuestos útiles como agentes antivirales, composiciones que comprenden estos compuestos y procesos para preparar los mismos. Reivindicación 1: Un compuesto de la fórmula (1) donde: Ar es un anillo aromático de 5- a 10-miembros que posee hasta 4 heteroátomos seleccionados de O, S, N(H), SO, y SO2, donde de 1 a 3 átomos de anillos son opcionalmente e independientemente sustituidos con J; R1 y R2 son independientemente: -alifático-(C1-12), -cicloalquil-(C3-10)- o -cicloalquenil-; [(3-10)- cicloalquil- o -cicloalquenil]-(C1-12)-alifático-; (C6-10)-aril-(C1-12)alifático-; (C6-10)-heteroaril-(C1-12)alifático-, donde hasta 3 átomos de C alifáticos en R1 y R2 pueden ser reemplazados por un heteroátomo seleccionado de O, N, S, SO, o SO2 en una disposición químicamente estable; donde cada uno de R1 y R2 es independientemente y opcionalmente sustituido con hasta 3 sustituyentes independientemente seleccionados de J; R3 y R3´ son independientemente H o (C1-12)-alifático, donde cualquier H es opcionalmente reemplazado con halógeno; donde cualquier átomo de C terminal de R3 es opcionalmente sustituido con sulfidrilo o hidroxi; o R3 es fenil o -CH2fenil, donde dicho grupo fenilo es opcionalmente sustituido con hasta 3 sustituyentes independientemente seleccionados de J; o R3 y R3´ junto con el átomo al cual se enlazan se encuentra un anillo de 3- a 6- miembros que poseen hasta dos heteroátomos seleccionados de N, NH, O, SO, y SO2; donde el anillo posee hasta 2 sustituyentes seleccionados independientemente de J; R4 y R4´ son independientemente: H, (C1-12)-alifático-, (C3-10)-cicloalquil- o -cicloalquenil-, (C3-10)-cicloalquil-(C1-12)-alifático-, (C6-10)-aril-, (C3-10)-heterociclil-; o (C5-10)-heteroaril-; donde hasta dos átomos de C alifáticos en R4 y R4´ pueden reemplazarse por un heteroátomo seleccionado de O, N; S, SO, y SO2; donde cada uno de R4 y R4´ es independientemente y opcionalmente sustituido con hasta 3 sustituyentes independientemente seleccionados de J; W es como se muestra en las fórmulas (2) donde cada R6 es independientemente: H, (C1-12)-alifático-, (C6-10)-aril-, (C6-10)-aril-(C1-12)alifático-, (C3-10)-cicloalquil- o cicloalquenil-, [(C3-10)-cicloalquil- o cicloalquenil]-(C1-12)-alifático- , (C3-10)-heterociclil-, (C3-10)-heterociclil-(C1-12)-alifático-, (C5-10)heteroaril-, o (C5-10)heteroaril-(C1-12)-alifático-, o dos grupos R6, que se enlazan al mismo átomo de N, forman junto con el átomo de N, un anillo heterocíclico de (C3-10); donde R6 es opcionalmente sustituido con hasta 3 J sustituyentes; donde cada R8 es independientemente -OR´; o los grupos R8 junto con el átomo de boro, es un anillo heterocíclico de (C3-10)-miembros que posee además del boro hasta 3 heteroátomos adicionales seleccionados de N, NH, O, SO, y SO2; T es (C1-12)-alifático-; (C6-10)-aril-, (C6-10)-aril-(C1-12)alifático-, (C5-10)heteroaril-, o (C5-10)heteroaril-(C1-12)-alifático-; donde cada T es opcionalmente sustituido con hasta 3 sustituyentes J; J es halógeno, OR´, -NO2, -CN, -CF3, -OCF3, -R´, oxo, tioxo, 1,2-metilendioxi, 1,2-etilendioxi, =N(R´), =N(OR´), -N(R´)2, -SR´, -SOR´, -SO2R´, -SO2N(R´)2, -SO3R´, -C(O)R´, -C(O)C(O)R´, -C(O)CH2C(O)R´, -C(S)R´, -C(S)OR´, -C(O)OR´, -C(O)C(O)OR´, - C(O)C(O)N(R´)2, -OC(O)R´, -C(O)N(R´)2, -OC(O)N(R´)2, -C(S)N(R´)2, -(CH2)0-2-NHC(O)R´, -N(R´)N(R´)COR´, -N(R´)N(R´)C(O)OR´, -N(R´)N(R´)CON(R´)2,.-N(R´)SO2R´, -N(R´)SO2N(R´)2, -N(R´)C(O)OR´, -N(R´)C(O)R´, -N(R´)C(S)R´, -N(R´)C(O)N(R´)2, - N(R´)C(S)N(R´)2, -N(COR´)COR´, -N(OR´)R´, -C(=NH)N(R´)2, -C(O)N(OR´)R´, -C(=NOR´)R´, -OP(O)(OR´)2, -P(O)(R´)2, -P(O)(OR´)2, o -P(O)(H)(OR´); R´ es H, (C1-12)-alifático-, (C3-10)-cicloalquil- o cicloalquenil-, [(C3-10)-cicloalquil o -cicloalquenil]- (C1-12)-alifático-, (C6-10)-aril-, (C6-10)-aril-(C1-12)alifático-, (C3-10)-heterociclil-, (C6-10)-heterociclil-(C1-12)alifático-, (C5-10)-heteroaril-, o (C5-10)-heteroaril-(C1-12)-alifático-; donde R´ es opcionalmente sustituido con hasta 3 J grupos; donde dos grupos R´ enlazados al mismo átomo forman un anillo no aromático o aromático de 3- a 10- miembros que poseen hasta 3 heteroátomos independientemente seleccionados de N, O, S, SO, o SO2, donde dicho anillo es opcionalmente fusionado a un (C6-10)aril, (C5-10)heteroaril, (C3-10)cicloalquil, o un (C3-10)heterociclil, donde cualquiera de los anillos posee hasta 3 sustituyentes seleccionados independientemente de J.
ARP040103191A 2003-09-05 2004-09-06 Inhibidores de proteasas de serina en particular proteasa ns3-ns4a del vhc AR045596A1 (es)

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Publication number Priority date Publication date Assignee Title
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