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 vhcInfo
- 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
- Authority
- AR
- Argentina
- Prior art keywords
- aliphatic
- heteroaryl
- cycloalkyl
- aryl
- independently
- Prior art date
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- 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
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- 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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- A—HUMAN NECESSITIES
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- 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
- A61K31/4439—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
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- 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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- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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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- 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
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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
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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
- A61P31/14—Antivirals for RNA viruses
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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
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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
- A61P31/20—Antivirals for DNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
- C04B35/632—Organic additives
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- C07D—HETEROCYCLIC COMPOUNDS
- 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
- 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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- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- 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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- C07K5/10—Tetrapeptides
- C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
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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.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US50067003P | 2003-09-05 | 2003-09-05 |
Publications (1)
Publication Number | Publication Date |
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AR045596A1 true AR045596A1 (es) | 2005-11-02 |
Family
ID=34434831
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP040103191A AR045596A1 (es) | 2003-09-05 | 2004-09-06 | Inhibidores de proteasas de serina en particular proteasa ns3-ns4a del vhc |
Country Status (20)
Country | Link |
---|---|
US (4) | US7378422B2 (es) |
EP (2) | EP1667998A2 (es) |
JP (2) | JP4767852B2 (es) |
KR (2) | KR20060073610A (es) |
CN (2) | CN1845920B (es) |
AR (1) | AR045596A1 (es) |
AU (1) | AU2004279800B9 (es) |
BR (1) | BRPI0414176A (es) |
CA (1) | CA2536436C (es) |
HK (1) | HK1095594A1 (es) |
IL (1) | IL173627A0 (es) |
MX (1) | MXPA06002476A (es) |
MY (1) | MY148123A (es) |
NO (1) | NO20061426L (es) |
NZ (2) | NZ580205A (es) |
PE (1) | PE20050374A1 (es) |
RU (2) | RU2440368C2 (es) |
TW (2) | TW201127828A (es) |
UY (1) | UY28500A1 (es) |
WO (1) | WO2005035525A2 (es) |
Families Citing this family (90)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HU227742B1 (en) | 1996-10-18 | 2012-02-28 | Vertex Pharma | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
WO2001074768A2 (en) * | 2000-04-03 | 2001-10-11 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
JP2003007697A (ja) * | 2001-06-21 | 2003-01-10 | Hitachi Kokusai Electric Inc | 半導体装置の製造方法、基板処理方法および基板処理装置 |
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2004
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- 2004-09-06 TW TW093127041A patent/TWI359147B/zh not_active IP Right Cessation
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