AR103969A1 - Inmunomoduladores - Google Patents
InmunomoduladoresInfo
- Publication number
- AR103969A1 AR103969A1 ARP160100725A ARP160100725A AR103969A1 AR 103969 A1 AR103969 A1 AR 103969A1 AR P160100725 A ARP160100725 A AR P160100725A AR P160100725 A ARP160100725 A AR P160100725A AR 103969 A1 AR103969 A1 AR 103969A1
- Authority
- AR
- Argentina
- Prior art keywords
- ring
- methyl
- alkyl
- optionally substituted
- independently selected
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/0005—Vertebrate antigens
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- A—HUMAN NECESSITIES
- 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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- 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
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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
- A61P31/04—Antibacterial agents
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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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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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- 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
- A61P37/04—Immunostimulants
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Abstract
Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o una sal de este aceptable desde el punto de vista farmacéutico, en donde: A se selecciona de los compuestos del grupo de fórmulas (2) en donde: la línea ondulada * indica el punto de unión al grupo carbonilo y la línea ondulada indica el punto de unión al átomo de nitrógeno; n es 0 ó 1; m es 1 ó 2; w es 0 ,1 ó 2; R¹⁴ y R¹⁵ se seleccionan independientemente de hidrógeno y metilo; R¹⁶ᵃ se selecciona de hidrógeno y C₁₋₆ alquilo; R¹⁶ se selecciona de -(C(R¹⁷ᵃ)₂)-C(O)-NR⁵⁰R⁵¹; en donde: cada R¹⁷ᵃ se selecciona independientemente de hidrógeno y C₁₋₆ alquilo; uno de R⁵⁰ y R⁵¹ se selecciona de hidrógeno y C₁₋₆ alquilo, y el otro se selecciona de -(CH₂)ₙX, C₁₋₆ alquilo, C₃₋₇ cicloalquilo, heterociclilo y fenilo, en donde el cicloalquilo se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados independientemente de C₁₋₃ alcoxi, C₁₋₃ alquilo, amino, ciano e hidroxi, o; R⁵⁰ y R⁵¹, junto con el átomo de nitrógeno al que están unidos, forman un anillo saturado o insaturado de cuatro, cinco, seis o siete miembros que contiene opcionalmente uno o dos heteroátomos adicionales seleccionados independientemente de nitrógeno, oxigeno y azufre; en donde el anillo se sustituye opcionalmente con uno, dos o tres grupos seleccionados de C₁₋₆ alcoxi, C₁₋₃ alquilo, ciano, halo, halo-C₁₋₃ alquilo, hidroxi, hidroxi(C₁₋₃ alquilo), -NR⁷⁰R⁷¹, oxo y fenilo; en donde fenilo se sustituye opcionalmente con uno, dos o tres grupos seleccionados independientemente de C₁₋₃ alcoxi, ciano y halo; n es 1 - 5; X se selecciona de un resto de fórmula (3), de fórmula (4), C₂₋₆ alcoximetilo, C₁₋₆ alcoxicarbonilmetilo, C₁₋₆ alquilsulfanilmetilo, C₁₋₆ alquilsulfonilmetilo, azidometilo, ter-butoximetilo, C₃₋₇ cicloalquilo, haloalcoximetilo, halometilo, heterociclilo, hidroximetilo, isopropoximetilo, (NR⁷⁰R⁷¹)metilo, fenilo, fenoximetilo, fenilsulfanilmetilo, uno de R⁷⁰ y R⁷¹ se selecciona de hidrógeno, C₁₋₆ alquilo e hidroxi-C₂₋₆ alquilo, y el otro se selecciona de C₁₋₆ alcoxicarbonilo, C₁₋₆ alquilcarbonilo, C₁₋₆ alquilsulfonilo e hidroxi-C₂₋₆ alquilo; la línea ondulada * indica el punto de unión al grupo carbonilo y la línea ondulada indica el punto de unión al átomo de nitrógeno; Rᶜ, Rᶠ, Rʰ, Rⁱ, Rᵐ y Rⁿ son hidrógeno; Rᵃ, Rᵉ, Rʲ y Rᵏ se seleccionan independientemente de hidrógeno y metilo; R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹² y R¹³ se seleccionan independientemente de una cadena lateral de aminoácido natural y una cadena lateral de aminoácido no natural o forman un anillo con el grupo R próximo correspondiente, como se describe más adelante; Rᵉ y Rᵏ pueden formar, cada uno, un anillo con el grupo R próximo correspondiente y los átomos a los que están unidos, seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, ciano, metilo, halo e hidroxi; Rᵇ es metilo, o Rᵇ y R², junto con los átomos a los que están unidos, forman un anillo seleccionado de azetidina, pirolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, ciano, metilo, halo e hidroxi; Rᵈ es hidrógeno o metilo, o Rᵈ y R⁴, junto con los átomos a los que están unidos, pueden formar un anillo seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, ciano, metilo, halo, hidroxi y fenilo; Rᵍ es hidrógeno o metilo, o Rᵍ y R⁷, junto con los átomos a los que están unidos, pueden formar un anillo seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, bencilo opcionalmente sustituido con un grupo halo, benciloxi, ciano, ciclohexilo, metilo, halo, hidroxi, isoquinoliniloxi opcionalmente sustituido con un grupo metoxi, quinoliniloxi opcionalmente sustituido con un grupo halo, y tetrazolilo; y en donde los anillos de pirrolidina y piperidina están opcionalmente fusionados con un grupo ciclohexilo, fenilo o indol; y Rˡ es metilo, o Rˡ y R¹², junto con los átomos a los que están unidos, forman un anillo seleccionado de azetidina y pirolidina, en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, ciano, metilo, halo e hidroxi. Reivindicación 5: Un método para mejorar, estimular y/o aumentar la respuesta inmunitaria en un sujeto que lo necesita; caracterizado porque comprende administrarle al sujeto una cantidad terapéuticamente eficaz de un compuesto de acuerdo con la reivindicación 1 o una sal de este terapéuticamente aceptable. Reivindicación 10: Un método para inhibir el crecimiento, la proliferación o la metástasis de células cancerosas en un sujeto que lo necesita; caracterizado porque comprende administrarle al sujeto una cantidad terapéuticamente eficaz de un compuesto de acuerdo con la reivindicación 1 o una sal de este terapéuticamente aceptable. Reivindicación 16: Un método para bloquear la interacción de PD-L1 con PD-1 y/o CD80 en un sujeto; caracterizado porque comprende administrar al sujeto una cantidad terapéuticamente eficaz de un compuesto de la reivindicación 1 o una sal de este terapéuticamente aceptable.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562134686P | 2015-03-18 | 2015-03-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR103969A1 true AR103969A1 (es) | 2017-06-14 |
Family
ID=55642894
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160100725A AR103969A1 (es) | 2015-03-18 | 2016-03-17 | Inmunomoduladores |
Country Status (16)
Country | Link |
---|---|
US (1) | US9809625B2 (es) |
EP (1) | EP3271373B1 (es) |
JP (1) | JP6797130B2 (es) |
KR (1) | KR102628640B1 (es) |
CN (1) | CN107428804B (es) |
AR (1) | AR103969A1 (es) |
AU (1) | AU2016233292A1 (es) |
BR (1) | BR112017019591A2 (es) |
CA (1) | CA2980147A1 (es) |
EA (1) | EA033739B1 (es) |
ES (1) | ES2910657T3 (es) |
IL (1) | IL254423A0 (es) |
MX (1) | MX2017011960A (es) |
SG (1) | SG11201707479YA (es) |
TW (1) | TW201702259A (es) |
WO (1) | WO2016149351A1 (es) |
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AU2016233292A1 (en) | 2017-11-09 |
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CN107428804A (zh) | 2017-12-01 |
EP3271373A1 (en) | 2018-01-24 |
US20160272680A1 (en) | 2016-09-22 |
IL254423A0 (en) | 2017-11-30 |
KR20170128489A (ko) | 2017-11-22 |
WO2016149351A1 (en) | 2016-09-22 |
US9809625B2 (en) | 2017-11-07 |
JP2018511590A (ja) | 2018-04-26 |
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