AR037976A1 - Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento. - Google Patents
Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento.Info
- Publication number
- AR037976A1 AR037976A1 ARP020105066A ARP020105066A AR037976A1 AR 037976 A1 AR037976 A1 AR 037976A1 AR P020105066 A ARP020105066 A AR P020105066A AR P020105066 A ARP020105066 A AR P020105066A AR 037976 A1 AR037976 A1 AR 037976A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het1
- het2
- cycloalkyl
- aryl
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940125366 antir retro viral Drugs 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 21
- 125000003118 aryl group Chemical group 0.000 abstract 18
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 15
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 5
- 125000003277 amino group Chemical group 0.000 abstract 4
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 3
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 abstract 3
- -1 C 2- alkenyl 6 Chemical group 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 abstract 2
- 125000005429 oxyalkyl group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 108010010369 HIV Protease Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 abstract 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 229940124522 antiretrovirals Drugs 0.000 abstract 1
- 239000003903 antiretrovirus agent Substances 0.000 abstract 1
- 125000005199 aryl carbonyloxy group Chemical group 0.000 abstract 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 abstract 1
- 125000005200 aryloxy carbonyloxy group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
- 150000003456 sulfonamides Chemical class 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
-
- 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
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/88—Nitrogen atoms, e.g. allantoin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D277/20—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
- C07D277/32—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 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
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D277/20—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
- C07D277/32—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 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
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D277/20—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
- C07D277/32—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 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
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
- C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
- C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
- C07C2603/18—Fluorenes; Hydrogenated fluorenes
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Reivindicación 1: Sulfonamidas que contienen fenilo sustituido con grupos heterocíclicos que tiene la fórmula (1) su N-óxido, sal, forma estereoisomérica, mezcla racémica, pro-fármaco, éster o metabolito, en los que: R1 y R8 son, cada uno, de manera independiente, hidrógeno, alquilo C1-6, alquenilo C2-6, arilalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, arilo, Het1, Het1 alquilo C1-6, Het2, Het2 alquilo C1-6; R1 también puede ser un radical de la fórmula (2) donde: R9, R10a y R10b son, cada uno, de manera independiente, hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4) aminocarbonilo, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 o alquilo C1-4 sustituido, de manera opcional, con arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4) aminocarbonilo, aminosulfonilo, alquil C1-4 S(O)t, hidroxi, ciano, halógeno o amino, mono- o disustituido de manera opcional donde los sustituyentes se seleccionan de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; donde R9, R10a y los átomos de carbono a los cuales están unidos también pueden formar un radical cicloalquilo C3-7; R11a es hidrógeno, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo, aminocarbonilo, mono- o disustituido de manera opcional, aminoalquil C1-4 carboniloxi mono- o di sustituido de manera opcional, alquiloxicarbonilo C1-4, ariloxicarbonilo, Het1 oxicarbonilo, Het2 oxicarbonilo, ariloxicarbonilalquilo C1-4, arilalquil C1-4 oxicarbonilo, alquilcarbonilo C1-4, cicloalquilcarbonilo C3-7, cicloalquil C3-7 alquiloxicarbonilo C1-4, cicloalquilcarboniloxi C3-7, carboxilalquil C1-4 carboniloxi, alquilcarboniloxi C1-4, arilalquilcarboniloxi C1-4, arilcarboniloxi, ariloxicarbonilox, Het1 carbonilo, Het1 carboniloxi, Het1 alquiloxicarbonilo C1-4, Het2 carboniloxi, Het2 alquilcarboniloxi C1-4, Het2 alquiloxicarboniloxi C1-4 o alquilo C1-4 sustituido de manera opcional con arilo, ariloxi, Het2 o hidroxi; donde los sustituyentes en los grupos amino se seleccionan cada uno, de manera independiente, de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; R11b es hidrógeno, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, arilo, Het1, Het2 o alquilo C1-4 sustituido, de manera opcional, con halógeno, hidroxi, alquilo C1-4S(=O)t, arilo, cicloalquilo C3-7, Het1, Het2, amino, mono- o disustituido, de manera opcional, donde los sustituyentes se seleccionan de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; donde R11b puede estar unido al resto de la molécula por medio de un grupo sulfonilo, R2 es hidrógeno o alquilo C1-6; L es -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-alcanodiilo C1-6-C(=O), -NR8-alcanodiilo C1-6-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 donde el grupo C(=O) o el grupo S(=O)2 está unido a la porción NR2; R3 es alquilo C1-6, arilo, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, o arilalquilo C1-4; R4 es hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo mono- o disustituido de manera opcional, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 o alquilo C1-6, donde el cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 y alquilo C1-6 pueden estar sustituidos, de manera opcional, con un sustituyente seleccionado de arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo mono- o disustituido de manera opcional, aminosulfonilo mono- o disustituido de manera opcional, alquil C1-4 S(=O)t, hidroxi, ciano, amino mono- o disustituido de manera opcional y halógeno, y donde los sustituyentes opcionales en la función amino se seleccionan, de manera independiente de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; t es 0, 1 o 2; cada t seleccionada de manera independiente es 0, 1 o 2; H arilo es un heterociclo monocíclico, bicíclico o tricíclico aromático que tiene de 3 a 14 miembros en el anillo que contiene en el anillo uno o más heteroátomos seleccionados de nitrógeno, oxígeno y azufre y que, pueden, de manera opcional, estar sustituidos en (1) uno o más átomos de carbono por alquilo C1-6, halógeno, hidroxi, amino mono- o disustituido de manera opcional, nitro, ciano, haloalquilo C1-6, carboxilo, cicloalquilo C3-7, aminocarbonilo mono- o disustituido de manera opcional, metiltio, metilsulfonilo, arilo, -(R7a)n-M-R7b, Het1 y Het2; donde los sustituyentes opcionales en cualquier función amino se seleccionan de manera independiente de R5 y -A-R6; y en (2) un átomo de nitrógeno si está presente, por hidroxi o -A-R6; A es alcanodiilo C1-6, -C(=O)-, -C(=S)-, -S(=O)2-, alcanodiilo C1-6 -C(=O)-, alcanodiilo C1-6 -C(=S)- o alcanodiilo C1-6 -S(=O)2; donde para aquellos grupos que contienen una porción alcanodiilo C1-6, la porción alcanodiilo C1-6 está unida al grupo amino; R5 es hidroxi, alquilo C1-6, Het1 alquilo C1-6, aminoalquilo C1-6 donde el grupo amino puede estar mono- o disustituido de manera opcional con alquilo C1-4; R6 es hidrógeno, alquiloxi C1-6, Het1, Het1 oxi, Het2 oxi, arilo, ariloxi o amino; y, en el caso en que -A- sea diferente de alcanodiilo C1-6, entonces, R6 también puede ser alquilo C1-6, Het1 alquilo C1-4, Het1 oxialquilo C1-4, Het2 alquilo C1-4, Het2 oxialquilo C1-4, arilalquilo C1-4, ariloxialquilo C1-4 o aminoalquilo C1-4; donde cada uno de os grupos amino en la definición de R6 pueden estar sustituidos, de manera opcional, con uno o más sustituyentes seleccionados de alquilo C1-4, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, arilo, arilcarbonilo, ariloxicarbonilo, Het1, Het2, arilalquilo C1-4, Het1 alquilo C1-4 o Het2 alquilo C1-4; R7a es alcanodiilo C1-8 sustituido, de manera opcional, por uno o más sustituyentes seleccionados de halógeno, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, arilo, arilcarbonilo, ariloxicarbonilo, Het1 o Het2; R7b es alquilo C1-8, sustituido, de manera opcional, con uno o más sustituyentes seleccionados de halógeno, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, arilo, arilcarbonilo, ariloxicarbonilo, Het1 o Het2; M se define como -C(=O)-, -O-C(=O)-, -C(=O)-O-, -CH2CHOH-, -CHOH-CH2-, -NR8-C(=O)-, -(C=O)-NR8-, -S(=O)2-, -O-, -S-, -O-S(=O)2-, -S(=O)2-O-, -NR8-S(=O)2 o -S(=O)2-R8-; n es 0 o 1. Fabricación de medicamentos como inhibidores de la proteasa del HIV de amplio espectro, los procesos de preparación, así como también las composiciones farmacéuticas que las comprenden, con otro agente antirretroviral.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01205115 | 2001-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037976A1 true AR037976A1 (es) | 2004-12-22 |
Family
ID=8181520
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020105066A AR037976A1 (es) | 2001-12-21 | 2002-12-20 | Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento. |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US7763641B2 (es) |
| EP (1) | EP1463502B1 (es) |
| JP (1) | JP4578101B2 (es) |
| KR (1) | KR100942743B1 (es) |
| CN (1) | CN100448444C (es) |
| AP (1) | AP1922A (es) |
| AR (1) | AR037976A1 (es) |
| AT (1) | ATE516029T1 (es) |
| AU (1) | AU2002361235B2 (es) |
| BR (1) | BR0215260A (es) |
| CA (1) | CA2470964C (es) |
| EA (1) | EA009556B1 (es) |
| HR (1) | HRP20040662B1 (es) |
| HU (1) | HUP0500164A3 (es) |
| IL (2) | IL162574A0 (es) |
| MX (1) | MXPA04006201A (es) |
| MY (1) | MY138657A (es) |
| NO (1) | NO328122B1 (es) |
| NZ (1) | NZ533665A (es) |
| PL (1) | PL216539B1 (es) |
| TW (1) | TWI336621B (es) |
| WO (1) | WO2003053435A1 (es) |
| ZA (1) | ZA200405784B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1581213A4 (en) * | 2002-12-18 | 2008-11-19 | Cytovia Inc | 3,5-DISUBSTITUTED 1,2,4-OXADIAZOLE AND ANALOGUE TO ACTIVATE CASPASE AND INTRODUCTION OF APOPTOSIS AND THEIR USE |
| EP1670448B1 (en) * | 2003-09-30 | 2007-11-21 | Tibotec Pharmaceuticals Ltd. | Hcv inhibiting sulfonamides |
| CA2566340C (en) * | 2004-05-07 | 2014-05-06 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| PT1856125E (pt) | 2005-02-25 | 2009-11-06 | Tibotec Pharm Ltd | Síntese de precursor de inibidor de proteases |
| WO2008004100A2 (en) | 2006-07-05 | 2008-01-10 | Pfizer Products Inc. | Therapeutic compounds |
| KR101483834B1 (ko) | 2009-12-23 | 2015-01-16 | 카트호리이케 유니버시타이트 로이펜 | 항바이러스 화합물 |
| WO2012031237A1 (en) | 2010-09-02 | 2012-03-08 | Purdue Research Foundation | Fused tricyclic ether carbamates and their use |
| EP2640705A2 (en) | 2010-11-15 | 2013-09-25 | Katholieke Universiteit Leuven | Novel antiviral compounds |
| CN105330675A (zh) | 2010-11-15 | 2016-02-17 | Viiv保健英国有限公司 | Hiv复制的抑制剂 |
| EP3192794A4 (en) * | 2014-09-11 | 2018-06-27 | Shionogi & Co., Ltd. | Sustained hiv protease inhibitor |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
| US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
| EP0715618B1 (en) | 1993-08-24 | 1998-12-16 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| PT721331E (pt) | 1993-10-01 | 2002-05-31 | Astrazeneca Ab | Processo i |
| ATE382041T1 (de) | 1995-01-20 | 2008-01-15 | Searle Llc | Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen |
| US5756533A (en) | 1995-03-10 | 1998-05-26 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| CN1530372A (zh) | 1995-03-10 | 2004-09-22 | G.D.ɪ����˾ | 杂环羰基氨基酸羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂 |
| US6150556A (en) | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US5705500A (en) | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| JPH09124630A (ja) | 1995-10-26 | 1997-05-13 | Kissei Pharmaceut Co Ltd | カルバミン酸テトラヒドロフリルエステル誘導体の製造方法 |
| AU7722296A (en) | 1995-11-15 | 1997-06-05 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| IL124935A (en) | 1996-05-20 | 2001-06-14 | Janssen Pharmaceutica Nv | Dispersible antifungal compositions comprising itraconazole with improved bioavailability |
| EP0969821B1 (en) | 1997-03-26 | 2003-06-04 | Janssen Pharmaceutica N.V. | Pellets having a core coated with an antifungal and a polymer |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| BR9814484A (pt) | 1997-12-24 | 2000-10-10 | Vertex Pharma | "pró-drogas de inibidores de aspartil protease" |
| WO1999033792A2 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
| ES2235492T3 (es) * | 1998-06-19 | 2005-07-01 | Vertex Pharmaceuticals Incorporated | Inhibidores de aspartil proteasa de tipo sulfonamida. |
| AU4828199A (en) | 1998-06-23 | 2000-01-10 | Board Of Trustees Of The University Of Illinois, The | Multi-drug resistant retroviral protease inhibitors and associated methods |
| CA2336160C (en) | 1998-06-23 | 2015-02-17 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Use of compounds for treating hiv |
-
2002
- 2002-12-20 HU HU0500164A patent/HUP0500164A3/hu unknown
- 2002-12-20 AU AU2002361235A patent/AU2002361235B2/en not_active Ceased
- 2002-12-20 EA EA200400828A patent/EA009556B1/ru not_active IP Right Cessation
- 2002-12-20 JP JP2003554192A patent/JP4578101B2/ja not_active Expired - Fee Related
- 2002-12-20 CN CNB028281667A patent/CN100448444C/zh not_active Expired - Fee Related
- 2002-12-20 US US10/499,221 patent/US7763641B2/en not_active Expired - Fee Related
- 2002-12-20 AT AT02796754T patent/ATE516029T1/de not_active IP Right Cessation
- 2002-12-20 EP EP02796754A patent/EP1463502B1/en not_active Expired - Lifetime
- 2002-12-20 PL PL370801A patent/PL216539B1/pl unknown
- 2002-12-20 WO PCT/EP2002/014839 patent/WO2003053435A1/en not_active Ceased
- 2002-12-20 TW TW091136901A patent/TWI336621B/zh not_active IP Right Cessation
- 2002-12-20 HR HRP20040662AA patent/HRP20040662B1/hr not_active IP Right Cessation
- 2002-12-20 MX MXPA04006201A patent/MXPA04006201A/es active IP Right Grant
- 2002-12-20 BR BR0215260-6A patent/BR0215260A/pt active Search and Examination
- 2002-12-20 KR KR1020047009850A patent/KR100942743B1/ko not_active Expired - Fee Related
- 2002-12-20 AR ARP020105066A patent/AR037976A1/es not_active Application Discontinuation
- 2002-12-20 IL IL16257402A patent/IL162574A0/xx unknown
- 2002-12-20 CA CA2470964A patent/CA2470964C/en not_active Expired - Fee Related
- 2002-12-20 AP APAP/P/2004/003083A patent/AP1922A/en active
- 2002-12-20 MY MYPI20024811A patent/MY138657A/en unknown
-
2004
- 2004-06-17 IL IL162574A patent/IL162574A/en not_active IP Right Cessation
- 2004-06-21 NZ NZ533665A patent/NZ533665A/en not_active IP Right Cessation
- 2004-07-20 NO NO20043114A patent/NO328122B1/no not_active IP Right Cessation
- 2004-07-20 ZA ZA2004/05784A patent/ZA200405784B/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR038240A1 (es) | Compuesto de piperidina, uso del mismo para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para su preparacion | |
| AR044045A1 (es) | Compuesto de piperidincarbonilpiperazina, composicion farmaceutica que lo comprende, su uso para la elaboracion de un medicamento y procedimiento para su preparacion | |
| EA200600527A1 (ru) | Активирующее ppar соединение и содержащая его фармацевтическая композиция | |
| AR068639A1 (es) | Derivados de biarilo | |
| AR035617A1 (es) | Compuestos derivados de fenetanolamina, combinaciones y formulaciones farmaceuticas de los mismos, proceso para su preparacion, su uso en la preparacion de medicamentos para el tratamiento o profilaxis de una condicion clinica para la cual se indica un agonista beta2 adreno-receptor e intermediarios | |
| AR081653A1 (es) | Inhibidores del virus de la hepatitis c | |
| AR037976A1 (es) | Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento. | |
| AR110139A1 (es) | COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV | |
| AR088218A1 (es) | Compuestos heterociclicos utiles como inhibidores de pi3k | |
| AR063602A1 (es) | Derivados de espiroindolinona, formulaciones farmaceuticas que los contienen y su uso en la obtencion de un medicamento para el tratamiento de trastornos oncologicos. | |
| AR062677A1 (es) | Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden | |
| AR041009A1 (es) | Compuestos heterociclicos nitrogenados que presentan actividad inhibitoria contra la integrasa del vih | |
| AR042542A1 (es) | Compuesto de benzazepina, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y proceso para su preparacion | |
| AR079689A1 (es) | Derivados de imidazo[1,2a]piridina, composiciones farmaceuticas que los comprenden y uso de los mismos en trastornos mieloproliferativos, leucemia y enfermedades inmunologicas e inflamatorias. | |
| AR070925A1 (es) | 4- hidroxipirimidina -5- carboxamida sustituidas, un procedimiento para el tratamiento preventivo de anemia, procedimiento para potenciar la produccion endogena de eritropoyetina, uso del compuesto en la fabricacion de un medicamento y composicion farmaceutica | |
| AR044152A1 (es) | Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad | |
| AR059957A1 (es) | DERIVADOS DE ESPIROINDOLINONA, MÉTODOS PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACÉUTICA QUE LOS CONTIENE Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DEL CÁNCER. | |
| AR032165A1 (es) | Carboxamidas heterociclicas, composiciones farmaceuticas, uso de dichas carboxamidas para preparar un medicamento como agentes antivirales y el uso in vitro para inhibir una dna polimerasa viral | |
| AR058073A1 (es) | Derivados de imidazol 5-il-pirimidina, procesos de obtencion, composiciones farmaceuticas y usos | |
| AR035970A1 (es) | 2-amino-benzoxazol sulfonamidas inhibidoras de amplio espectro de la hiv proteasa, composicion farmaceutica, metodo "in vitro" para inhibir la replicacion retroviral, y utilizacion de estos compuestos en la manufactura de medicamentos | |
| AR019790A2 (es) | Compuestos derivados de la eritromicina, composiciones que los contienen. uso para preparar un medicamento | |
| AR051984A1 (es) | Compuestos heterociclicos como inhibidores del factor viia | |
| AR038404A1 (es) | Derivados de nicotinamida utiles como inhibidores de pde4, procedimiento para la preparacion del compuesto y composicion farmaceutica que lo incluye | |
| AR079967A1 (es) | Derivados de acido 3-heteroaroilamino-propionico sustituidos con oxigeno y su uso como productos farmaceuticos | |
| AR044518A1 (es) | Inhibidores de integrasa de hiv |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |