AR078396A1 - Inhibidores de la polimerasa virica y composiciones farmaceuticas que los contienen - Google Patents
Inhibidores de la polimerasa virica y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR078396A1 AR078396A1 ARP100103411A ARP100103411A AR078396A1 AR 078396 A1 AR078396 A1 AR 078396A1 AR P100103411 A ARP100103411 A AR P100103411A AR P100103411 A ARP100103411 A AR P100103411A AR 078396 A1 AR078396 A1 AR 078396A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- het
- aryl
- optionally substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 43
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 15
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 125000005843 halogen group Chemical group 0.000 abstract 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 10
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 7
- 125000005842 heteroatom Chemical group 0.000 abstract 7
- 125000004043 oxo group Chemical group O=* 0.000 abstract 7
- -1 -C1-6 alkyl halo Chemical group 0.000 abstract 5
- 229910052760 oxygen Inorganic materials 0.000 abstract 5
- 229910052717 sulfur Inorganic materials 0.000 abstract 5
- 125000002947 alkylene group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 3
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 241000711549 Hepacivirus C Species 0.000 abstract 1
- 101800001554 RNA-directed RNA polymerase Proteins 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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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- 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
- A61K31/13—Amines
- A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
-
- 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
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
- C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
- C07C211/29—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
-
- 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
- C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C233/11—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having carbon atoms of carboxamide groups, amino groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C251/48—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino 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
- 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
- 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
- C07C255/59—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 the carbon skeleton being further substituted by singly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D401/14—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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Gastroenterology & Hepatology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Son utiles como inhibidores de la polimerasa NS5B del virus de la hepatitis C. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) en la que X se selecciona entre O, CH2 y S; R2 es cicloalquilo C3-6, arilo o Het, estando todos ellos opcionalmente sustituidos con 1 a 5 sustituyentes R20, donde R20 se selecciona independientemente en cada caso entre: a) halo, ciano, oxo o nitro; b) R7, -C(=O)-R7, -C(=O)OR7, -OR7, -SR7, -SOR7, -SO2R7, -alquileno C1-6-R7, -alquileno C1-6-C(=O)R7, -alquileno C1-6-C(=O)OR7, -alquileno C1-6-OR7, -alquileno C1-6-SR7, -alquileno C1-6-SOR7 o -alquileno C1-6-SO2R7; donde R7 se selecciona independientemente en cada caso entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo C3-7, espirocicloalquilo C3-7 que contiene opcionalmente de 1 a 3 heteroátomos seleccionados entre N, O y S, arilo y Het; donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6 y cicloalquilo C3-7 están opcionalmente sustituidos con 1 a 5 sustituyentes, cada uno seleccionado independientemente entre -OH, oxo, -alquilo C1-6 (opcionalmente sustituido con -O-alquilo C1-6, halo, -haloalquilo C1-6, cicloalquilo C3-7, -O-alquilo C1-6, ciano, COOH, - N(R8)R9, -C(=O)N(R8)R9, espirocicloalquilo C3-7 que contiene opcionalmente de 1 a 3 heteroátomos seleccionados entre N, O y S, arilo, -alquil C1-6-arilo, Het y -alquil C1-6-Het; y donde cada uno del arilo y Het está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno seleccionado independientemente entre i) halo, ciano, oxo, tioxo, imino, -OH, -COOH, -O-alquilo C1-6, -Ohaloalquilo C1-6, cicloalquilo C3-7, haloalquilo C1-6, -C(=O)-alquilo C1-6, SO2NH2, -SO2-NHalquilo C1-6, -SO2-N(alquilo C1-6)2, -SO2alquilo C1-6, -C(=O)-NH2, -C(=O)-NHalquilo C1-4, -C(=O)-N(alquilo C1-4)2, -C(=O)-NHcicloalquilo C3-7, -C(=O)N(alquil C1-4)-cicloalquilo C3-7, -NH2, -NHalquilo C1-4, -N(alquilo C1-4)2, -NHcicloalquilo 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-halogenoalquil C1-6 o -O-alquilo C1-6; y iii) arilo o Het, donde cada uno de los grupos arilo y Het está opcionalmente sustituido con halo, OH, alquilo C1-6 o -O-alquilo C1-6; y c) -N(R8)R9, -C(=O)-N(R8)R9, -O-C(=O)-N(R8)R9, -SO2-N(R8)R9, -alquileno C1-6-N(R8)R9, -alquileno C1-6)-C(=O)-N(R8)R9, -alquileno C1-6-O-C(=O)-N(R8)R9, -alquileno C1-6-SO2-N(R8)R9 o -alquileno C1-6-NR9-SO2-N(R8)R9 donde el alquileno C1-6 está opcionalmente sustituido con 1 o 2 sustituyentes, cada uno seleccionado independientemente 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(alquilC1-4)-cicloalquilo C3-7 y -N(alquilo C1-4)2; R8 se selecciona independientemente en cada caso entre H, alquilo C1-6, cicloalquilo C3-7, -C(=O)R7 y -C(=O)OR7; y R9 se selecciona independientemente en cada caso entre halo, ciano, R7, OR7, -alquileno C1-6-R7, -SO2R7, -C(=O)R7, -OC(=O)R7, -C(=O)OR7 y -C(=O)N(R8)R7; 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 contiene opcionalmente de 1 a 3 heteroátomos, cada uno seleccionado independientemente entre N, O y S, 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; donde el heterociclo está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno seleccionado independientemente entre alquilo C1-6 opcionalmente sustituido con OH, haloalquilo C1-6, halo, oxo, -OH, SH, -O-alquilo C1-6, -S-alquilo C1-6, cicloalquilo C3-7, -NH2, -NHalquilo C1-6, -N(alquilo C1-6)2, -NHcicloalquilo C3-7, -N(alquil C1-4)-cicloalquilo C3-7, -C(=O)alquilo C1-6-cicloalquilo C3-7 y -NHC(=O)-alquilo C1-6; R3 se selecciona entre H, halo, alquilo C1-6, haloalquilo C1-6, -O-alquilo C1-6, -Salquilo C1-6, ciano, -NH2, -NHalquilo C1-6 y -N(alquilo C1-6)2; R5 se selecciona entre H, alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, -O-alquilo C1-6, -S-alquilo C1-6, ciano, -NH2, -NHalquilo C1-6, -N(alquilo C1-6)2, -NHC(=O)-alquilo C1-3, arilo, aril-alquil C1-6-, Het o Het-alquil C1-6-; donde el alquilo C1-6, arilo, aril-alquil C1-6-, Het o Het-alquil C1-6- están opcionalmente sustituidos con 1 a 4 sustituyentes, cada uno seleccionado independientemente entre alquilo C1-6, halo, -OH, -COOH, -O-alquilo C1-6, -C(=O)-alquilo C1-4, -C(=O)-O-alquilo C1-6, ciano, -NH2, -NHalquilo C1-6 y -N(alquilo C1-6)2; R6 se selecciona entre alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-7, arilo y Het, donde dicho R6 puede estar opcionalmente sustituido con 1 a 6 sustituyentes R21, donde R21 se selecciona independientemente en cada caso entre: c) halo, NH2, NO2, ciano, azido u oxo; d) R210, OR210, NR210R211, SR210, SOR210, SO2R210, C(=O)R210, C(=O)OR210, C(=O)NR210R211, NR211C(=O)R212, NR211C(=O)OR212, NR211C(=O)NR211R212, NR211SO2R210, NR211SO2NR210R212 y SO2NR210R211; donde 210 se selecciona entre H, alquilo C1-8, haloalquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-7, cicloalquenilo C5-7, espirocicloalquilo C3-7 que contiene opcionalmente de 1 a 3 heteroátomos seleccionados entre N, O y S, C(=O)R211, C(=O)OR211, arilo y Het, pudiendo estar todos ellos opcionalmente sustituidos con 1 a 6 sustituyentes seleccionados entre OH, NH2, ciano, oxo, NO2, halo, R212, OR211, SR211, NR211R212, NR211C(=O)R212, NR211C(=O)OR212, NR211C(=O)NR211R212, NR211SO2R210, NR211SO2NR210R212, C(=O)R211, C(=O)OR211, C(=O)NR211R212, y donde R211 se selecciona entre H, alquilo C1-6 y cicloalquilo C3-7; y donde R212 se selecciona entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, -O-alquilo C1-6, cicloalquilo C3-7, cicloalquenilo C3-7, arilo y Het, estando todos ellos opcionalmente sustituidos con 1 a 6 sustituyentes seleccionados entre OH, NH2, ciano, oxo, NO2, halo, alquilo C1-6, cicloalquilo C3-7, haloalquilo C1-6, O-alquilo C1-6, S-alquilo C1-6, NHalquilo C1-6, N(alquilo C1-6)2, arilo y Het, donde el arilo y Het pueden estar opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados entre OH, halo, alquilo C1-3 y -O-alquilo C1-3; o R210 y R211, o R211 y R212, junto con el N al que están unidos, se unen para formar un heterociclo de 4 a 7 miembros que además contiene opcionalmente de 1 a 3 heteroátomos, cada uno seleccionado independientemente entre N, O y S, 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 donde el heterociclo está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno seleccionado independientemente entre alquilo C1-6, halogenoalquilo C1-6, halogeno, oxo, -OH, SH, -O-alquilo C1-6, S-alquilo C1-6, cicloalquilo C3-7, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NH-cicloalquilo C3-7, -N(alquil C1-4)-cicloalquilo C3-7, -C(=O)-alquilo C1-6 y -NHC(=O)-alquilo C1-6; o una sal del mismo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US24378309P | 2009-09-18 | 2009-09-18 | |
US35482010P | 2010-06-15 | 2010-06-15 |
Publications (1)
Publication Number | Publication Date |
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AR078396A1 true AR078396A1 (es) | 2011-11-02 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP100103411A AR078396A1 (es) | 2009-09-18 | 2010-09-17 | Inhibidores de la polimerasa virica y composiciones farmaceuticas que los contienen |
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US (1) | US20110230465A1 (es) |
EP (1) | EP2477976A4 (es) |
JP (1) | JP2013504604A (es) |
AR (1) | AR078396A1 (es) |
TW (1) | TW201121945A (es) |
WO (1) | WO2011032277A1 (es) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
CN101031569B (zh) | 2004-05-13 | 2011-06-22 | 艾科斯有限公司 | 作为人磷脂酰肌醇3-激酶δ抑制剂的喹唑啉酮 |
US9492449B2 (en) | 2008-11-13 | 2016-11-15 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
ES2674719T3 (es) | 2008-11-13 | 2018-07-03 | Gilead Calistoga Llc | Terapias para neoplasias hematológicas |
AU2010239312A1 (en) * | 2009-04-20 | 2011-11-10 | Gilead Calistoga Llc | Methods of treatment for solid tumors |
MX2012000817A (es) | 2009-07-21 | 2012-05-08 | Gilead Calistoga Llc | Tratamiento para desordenes del higado con inhibidores pi3k. |
CN103889963B (zh) * | 2011-08-12 | 2016-01-20 | 南方研究所 | 喹唑啉酮类似物以及喹唑啉酮类似物在用于治疗或预防某些病毒感染中的应用 |
WO2013113863A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
WO2013113773A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
WO2013113720A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
WO2013113776A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
WO2013113716A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
WO2013113791A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
WO2013113715A1 (en) | 2012-02-03 | 2013-08-08 | Basf Se | Fungicidal pyrimidine compounds |
UY34656A (es) | 2012-03-05 | 2013-10-31 | Gilead Calistoga Llc | Polimorfos de (s)?2?(1?(9h?purin?6?ilamino)propil)?5?fluor?3?fenilquinazolin?4(3h)?ona, composición y método de preparación |
WO2013135672A1 (en) | 2012-03-13 | 2013-09-19 | Basf Se | Fungicidal pyrimidine compounds |
MX2015014407A (es) | 2013-04-15 | 2015-12-07 | Du Pont | Amidas fungicidas. |
EA201690990A1 (ru) | 2013-12-20 | 2016-11-30 | Джилид Калистога Ллс | Способы получения ингибиторов фосфатидилинозитол-3-киназы |
EP3083623A1 (en) | 2013-12-20 | 2016-10-26 | Gilead Calistoga LLC | Polymorphic forms of a hydrochloride salt of (s) -2-(9h-purin-6-ylamino) propyl) -5-fluoro-3-phenylquinazolin-4 (3h) -one |
BR112016028642A2 (pt) | 2014-06-13 | 2017-08-22 | Gilead Sciences Inc | composto, composição farmacêutica, método de tratamento de uma doença ou condição, método de inibição da atividade de um polipeptídeo de fosfatidilinositol 3-quinase, método de inibição de reações imunes ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, e, uso de um composto, de um sal, de um isômero ou de uma mistura farmaceuticamente aceitável do mesmo. |
MA41598A (fr) | 2015-02-25 | 2018-01-02 | Constellation Pharmaceuticals Inc | Composés thérapeutiques de pyridazine et leurs utilisations |
JP7268049B2 (ja) | 2018-03-08 | 2023-05-02 | インサイト・コーポレイション | PI3K-γ阻害剤としてのアミノピラジンジオール化合物 |
WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002517486A (ja) * | 1998-06-12 | 2002-06-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | p38のインヒビター |
EA007538B1 (ru) * | 2000-12-11 | 2006-10-27 | Туларик Инк. | Антагонисты cxcr3 |
US7816348B2 (en) * | 2006-02-03 | 2010-10-19 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
EP2054388A4 (en) * | 2006-08-17 | 2009-10-28 | Boehringer Ingelheim Int | VIRAL POLYMERASE HEMMER |
WO2009018656A1 (en) * | 2007-08-03 | 2009-02-12 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
-
2010
- 2010-09-16 WO PCT/CA2010/001443 patent/WO2011032277A1/en active Application Filing
- 2010-09-16 JP JP2012529077A patent/JP2013504604A/ja active Pending
- 2010-09-16 EP EP10816523A patent/EP2477976A4/en not_active Withdrawn
- 2010-09-16 US US12/883,677 patent/US20110230465A1/en not_active Abandoned
- 2010-09-17 TW TW099131764A patent/TW201121945A/zh unknown
- 2010-09-17 AR ARP100103411A patent/AR078396A1/es unknown
Also Published As
Publication number | Publication date |
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EP2477976A4 (en) | 2013-03-13 |
WO2011032277A1 (en) | 2011-03-24 |
US20110230465A1 (en) | 2011-09-22 |
JP2013504604A (ja) | 2013-02-07 |
TW201121945A (en) | 2011-07-01 |
EP2477976A1 (en) | 2012-07-25 |
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