AR120481A1 - Compuestos útiles como inhibidores de la proteína helios - Google Patents
Compuestos útiles como inhibidores de la proteína heliosInfo
- Publication number
- AR120481A1 AR120481A1 ARP200103178A ARP200103178A AR120481A1 AR 120481 A1 AR120481 A1 AR 120481A1 AR P200103178 A ARP200103178 A AR P200103178A AR P200103178 A ARP200103178 A AR P200103178A AR 120481 A1 AR120481 A1 AR 120481A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- fluoroalkyl
- independently
- alkoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 16
- -1 azocanyl Chemical group 0.000 abstract 13
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 6
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000003386 piperidinyl group Chemical group 0.000 abstract 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 3
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000002393 azetidinyl group Chemical group 0.000 abstract 2
- 125000002541 furyl group Chemical group 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 2
- 125000003944 tolyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000003725 azepanyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005959 diazepanyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl 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
- C07D401/14—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
-
- 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
- A61K31/435—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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
-
- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Un compuesto de la fórmula (1) o una sal del mismo, en donde: Z es CR⁶R⁶ o C=O; el anillo A es: un compuesto seleccionado del grupo de fórmulas (2); R¹ es -(CRᶻRᶻ)₁₋₂NR¹ᵃR¹ᵇ; R¹ᵃ es hidrógeno, alquilo C₁₋₆, fluoroalquilo C₁₋₄, cianoalquilo C₁₋₃, hidroxialquilo C₁₋₆, -(CH₂)₁₋₃O(alquilo C₁₋₃), -(CH₂)₁₋₃S(O)₂(alquilo C₁₋₃), -(CH₂)₁₋₃C₍O₎O₍ₐₗqᵘⁱₗₒ C₁₋₃), -(CH₂)₁₋₃NRˣRˣ, -(CH₂)₁₋₃C₍O₎NRˣRˣ, -(CH₂)₁₋₃NRˣC(O)(alquilo C₁₋₃), -C(O)(alquilo C₁₋₃), -CH(fenil)(hidroxialquilo C₁₋₂), -CRˣRˣCRˣ(fenil)₂, R¹ᶜ, -(CRˣRˣ)₁₋₃R¹ᶜ, -(CRˣRˣ)₁₋₃OR¹ᶜ, o -C(O)R¹ᶜ; R¹ᵇ es hidrógeno, alquilo C₁₋₃, o -CH₂(fenil); o R¹ᵃ y R¹ᵇ junto con el átomo de nitrógeno al que están unidos, se unen para formar un grupo cíclico seleccionado de azaspiro[2.5]octanilo, azepanilo, azetidinilo, azocanilo, diazepanilo, dioxidotiomorfolinilo, isoindolinilo, morfolinilo, octahidrociclopenta[b]pirrolilo, octahidropirrolo[3,4-c]pirrolilo, oxaazabiciclo[2.2.1]heptanilo, piperazinonilo, piperazinilo, piperidinonilo, piperidinilo, pirrolidinilo, pirrolidinonilo, y tetrahidroisoquinolinilo, cada uno sustituido por cero a 1 R¹ᵈ y cero a 2 R¹ᵉ; R¹ᶜ es cicloalquilo C₃₋₇, fenilo, oxetanilo, azetidinilo, furanilo, piranilo, pirrolilo, pirrolidinilo, pirrolidinonilo, pirazolilo, imidazolilo, indazolilo, tiazolilo, piperidinilo, piridinilo, tetrahidrofuranilo, tetrahidropiranilo, morfolinilo, dioxotetrahidrotiopiranilo, dioxidotetrahidrotiofenilo, benzo[d]tiazolilo, naftalenilo, quinolinilo, o quinoxalinilo, cada uno sustituido por cero a 2 sustituyentes independientemente seleccionados F, Cl, -CN, -OH, alquilo C₁₋₃, fluoroalquilo C₁₋₃, hidroxialquilo C₁₋₃, alcoxi C₁₋₃, fluoroalcoxi C₁₋₃, -C(O)O(alquilo C₁₋₃), -NRʸRʸ, -S(O)₂(alquilo C₁₋₃), -S(O)₂NRˣRˣ, -CH₂(fenilo), -NO₂, cicloalquilo C₃₋₆, imidazolilo, y fenilo; R¹ᵈ es alquilo C₁₋₄, fluoroalquilo C₁₋₂, alcoxi C₁₋₃, -NRʸRʸ, -NRˣC(O)(alquilo C₁₋₃), -C(O)(alquilo C₁₋₃), -C(O)NRʸRʸ, -CH₂(fenilo), -CH₂(metilpirrolidinilo), -CH₂(benzo[d][1,3]dioxolilo), -CH(fenilo)₂, -C(O)(tetrahidrofuranilo), -C(O)(furanilo), -S(O)₂(metilfenilo), fenilo, metilfenilo, aminofenilo, piperidinilo, pirazinilo, piridinilo, pirimidinilo, pirrolidinilo, o dihidrobenzo[d]imidazolonilo; R¹ᵉ es CH₃; cada R² es independientemente halógeno, -CN, alquilo C₁₋₃, fluoroalquilo C₁₋₃, alcoxi C₁₋₃, o fluoroalcoxi C₁₋₃; NR₂ (R = H, alquilo C₁₋₃), opcionalmente sustituido fenilo, opcionalmente sustituido heteroarilo; R³ es R¹ᵃ; cada R⁴ es independientemente halógeno, -CN, alquilo C₁₋₃, fluoroalquilo C₁₋₃, alcoxi C₁₋₃, o fluoroalcoxi C₁₋₃; cada R⁴ es independientemente halógeno, -CN, -OH, alquilo C₁₋₃, fluoroalquilo C₁₋₃, alcoxi C₁₋₃, fluoroalcoxi C₁₋₃, o -NRʸRʸ; R⁵ es hidrógeno, F, o alquilo C₁₋₃; cada R⁶ es independientemente hidrógeno o alquilo C₁₋₃; cada Rˣ es independientemente H o -CH₃; cada Rʸ es independientemente H o alquilo C₁₋₄; cada Rᶻ es independientemente H o -CH₃; o dos Rᶻ unido al mismo átomo de carbono, forman un anillo carbocíclico de 3 a 6 miembros o un anillo heterocíclico de 3 a 6 miembros; m es cero, 1, ó 2; y n es cero, 1, 2, ó 3.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201962937350P | 2019-11-19 | 2019-11-19 |
Publications (1)
Publication Number | Publication Date |
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AR120481A1 true AR120481A1 (es) | 2022-02-16 |
Family
ID=73834595
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP200103178A AR120481A1 (es) | 2019-11-19 | 2020-11-18 | Compuestos útiles como inhibidores de la proteína helios |
Country Status (13)
Country | Link |
---|---|
US (1) | US11548870B2 (es) |
EP (1) | EP4061812A1 (es) |
JP (1) | JP2023503052A (es) |
KR (1) | KR20220103753A (es) |
CN (1) | CN114728950A (es) |
AR (1) | AR120481A1 (es) |
AU (1) | AU2020387392A1 (es) |
BR (1) | BR112022009514A2 (es) |
CA (1) | CA3158976A1 (es) |
IL (1) | IL293027A (es) |
MX (1) | MX2022005839A (es) |
TW (1) | TWI836159B (es) |
WO (1) | WO2021101919A1 (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
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TW202140441A (zh) * | 2020-03-23 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 經取代之側氧基異吲哚啉化合物 |
US20230271940A1 (en) * | 2020-08-03 | 2023-08-31 | Novartis Ag | Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
KR20230167067A (ko) * | 2021-04-05 | 2023-12-07 | 브리스톨-마이어스 스큅 컴퍼니 | 암의 치료를 위한 피리디닐 치환된 옥소이소인돌린 화합물 |
CN115504963A (zh) * | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | 一种c-Myc蛋白降解剂 |
WO2023283425A1 (en) | 2021-07-09 | 2023-01-12 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
AU2022375782A1 (en) | 2021-10-28 | 2024-05-02 | Gilead Sciences, Inc. | Pyridizin-3(2h)-one derivatives |
CN118201941A (zh) | 2021-10-29 | 2024-06-14 | 吉利德科学公司 | Cd73化合物 |
CA3237577A1 (en) | 2021-12-22 | 2023-06-29 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
US20240124412A1 (en) | 2021-12-22 | 2024-04-18 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Parp7抑制劑 |
WO2023154417A1 (en) * | 2022-02-09 | 2023-08-17 | C4 Therapeutics, Inc. | Morphic forms of cft7455 and methods of manufacture thereof |
WO2023178181A1 (en) | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
WO2023205719A1 (en) | 2022-04-21 | 2023-10-26 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
WO2024006929A1 (en) | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Cd73 compounds |
WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
WO2024137852A1 (en) | 2022-12-22 | 2024-06-27 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
Family Cites Families (67)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE69717831T3 (de) | 1996-07-24 | 2018-08-30 | Celgene Corp. | Substituierte 2-(2,6-dioxopiperidin-3-yl)-phthalimide und -1-oxoisoindoline und verfahren zur reduzierung des tnf-alpha-spiegels |
US20030045552A1 (en) | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
JP4494013B2 (ja) | 2001-08-06 | 2010-06-30 | ザ チルドレンズ メディカル センター コーポレイション | 窒素置換サリドマイド誘導体の合成及び抗腫瘍活性 |
TWI309240B (en) | 2004-09-17 | 2009-05-01 | Hoffmann La Roche | Anti-ox40l antibodies |
JP5238936B2 (ja) | 2005-03-25 | 2013-07-17 | ジーアイティーアール,インク. | Gitr結合分子およびその使用 |
KR101562549B1 (ko) | 2005-05-10 | 2015-10-23 | 인사이트 홀딩스 코포레이션 | 인돌아민 2,3-디옥시게나제의 조절제 및 이의 사용방법 |
CN104356236B (zh) | 2005-07-01 | 2020-07-03 | E.R.施贵宝&圣斯有限责任公司 | 抗程序性死亡配体1(pd-l1)的人单克隆抗体 |
CA2634198C (en) | 2005-12-20 | 2014-06-03 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
WO2008036642A2 (en) | 2006-09-19 | 2008-03-27 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
JP5932217B2 (ja) | 2007-07-12 | 2016-06-08 | ジーアイティーアール, インコーポレイテッド | Gitr結合分子を使用する併用療法 |
EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
CA2932121A1 (en) | 2007-11-30 | 2009-06-11 | Newlink Genetics Corporation | Ido inhibitors |
DK2234620T3 (en) | 2008-01-03 | 2016-06-06 | Université D'aix-Marseille | Triple therapy used for treatment of an hiv-infected patient |
WO2009137095A2 (en) | 2008-05-08 | 2009-11-12 | The Johns Hopkins University | Compositions and methods for modulating an immune response |
AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
EP4169951A1 (en) | 2008-12-09 | 2023-04-26 | F. Hoffmann-La Roche AG | Anti-pd-l1 antibodies and their use to enhance t-cell function |
JP5561577B2 (ja) | 2009-07-01 | 2014-07-30 | 国立大学法人 名古屋工業大学 | 光学活性3’−フルオロサリドマイド誘導体の製造方法 |
US8709424B2 (en) | 2009-09-03 | 2014-04-29 | Merck Sharp & Dohme Corp. | Anti-GITR antibodies |
WO2011056652A1 (en) | 2009-10-28 | 2011-05-12 | Newlink Genetics | Imidazole derivatives as ido inhibitors |
CA2780692C (en) | 2009-12-10 | 2018-09-11 | F. Hoffmann-La Roche Ag | Antibodies binding preferentially human csf1r extracellular domain 4 and their use |
SG183847A1 (en) | 2010-03-04 | 2012-10-30 | Macrogenics Inc | Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof |
CN102918061B (zh) | 2010-03-05 | 2016-06-08 | 霍夫曼-拉罗奇有限公司 | 针对人csf-1r的抗体及其用途 |
RU2617971C2 (ru) | 2010-03-05 | 2017-04-28 | Ф.Хоффманн-Ля Рош Аг | Антитела против csf-1r человека и их применение |
US8206715B2 (en) | 2010-05-04 | 2012-06-26 | Five Prime Therapeutics, Inc. | Antibodies that bind colony stimulating factor 1 receptor (CSF1R) |
EP2614082B1 (en) | 2010-09-09 | 2018-10-03 | Pfizer Inc | 4-1bb binding molecules |
NO2694640T3 (es) | 2011-04-15 | 2018-03-17 | ||
WO2012145493A1 (en) | 2011-04-20 | 2012-10-26 | Amplimmune, Inc. | Antibodies and other molecules that bind b7-h1 and pd-1 |
SG11201402603WA (en) | 2011-11-28 | 2014-06-27 | Merck Patent Gmbh | Anti-pd-l1 antibodies and uses thereof |
WO2013087699A1 (en) | 2011-12-15 | 2013-06-20 | F. Hoffmann-La Roche Ag | Antibodies against human csf-1r and uses thereof |
RU2014136332A (ru) | 2012-02-06 | 2016-03-27 | Дженентек, Инк. | Композиции и способы применения ингибиторов csf1r |
AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
WO2013169264A1 (en) | 2012-05-11 | 2013-11-14 | Five Prime Therapeutics, Inc. | Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r) |
AR091649A1 (es) | 2012-07-02 | 2015-02-18 | Bristol Myers Squibb Co | Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos |
TWI713436B (zh) | 2012-08-31 | 2020-12-21 | 美商戊瑞治療有限公司 | 用結合群落刺激因子1受體(csf1r)之抗體治療病狀之方法 |
WO2015107196A1 (en) | 2014-01-20 | 2015-07-23 | Institut Curie | Use of thalidomide or analogs thereof for preventing neurologic disorders induced by brain irradiation |
US9499514B2 (en) * | 2014-07-11 | 2016-11-22 | Celgene Corporation | Antiproliferative compounds and methods of use thereof |
MX2017014567A (es) | 2015-05-22 | 2018-06-28 | Biotheryx Inc | Compuestos que tienen como dianas a proteinas, composiciones, metodos y usos de los mismos. |
AU2016270442C1 (en) | 2015-06-04 | 2022-06-02 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
GB201516243D0 (en) | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
WO2017117118A1 (en) | 2015-12-28 | 2017-07-06 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases |
WO2017161119A1 (en) | 2016-03-16 | 2017-09-21 | H. Lee Moffitt Cancer Center & Research Institute, Inc. | Small molecules against cereblon to enhance effector t cell function |
RU2021102253A (ru) | 2016-04-06 | 2021-03-03 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Деструкторы белка mdm2 |
AU2017254711B2 (en) | 2016-04-22 | 2021-01-21 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 8 (CDK8) by conjugation of CDK8 inhibitors with E3 ligase ligand and methods of use |
WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
WO2018052945A1 (en) | 2016-09-13 | 2018-03-22 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines as bet protein degraders |
CA3038979A1 (en) | 2016-10-11 | 2018-04-19 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
US11458123B2 (en) | 2016-11-01 | 2022-10-04 | Arvinas Operations, Inc. | Tau-protein targeting PROTACs and associated methods of use |
RU2750484C2 (ru) | 2016-12-01 | 2021-06-28 | Эрвинэс Оперейшнс, Инк. | Производные тетрагидронафталина и тетрагидроизохинолина в качестве разрушителей эстрогенового рецептора |
US10040804B2 (en) | 2016-12-21 | 2018-08-07 | Biotheryx, Inc. | Compounds targeting proteins, compositions, methods, and uses thereof |
US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
JP2020504741A (ja) | 2016-12-23 | 2020-02-13 | アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. | Raf(急速進行性線維肉腫)ポリペプチドの標的分解のための化合物および方法 |
CA3047586A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas Operations, Inc. | Egfr proteolysis targeting chimeric molecules and associated methods of use |
TWI793151B (zh) * | 2017-08-23 | 2023-02-21 | 瑞士商諾華公司 | 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途 |
JP2021501570A (ja) * | 2017-10-18 | 2021-01-21 | ノバルティス アーゲー | 選択的タンパク質分解のための組成物及び方法 |
JP2021512153A (ja) | 2018-01-26 | 2021-05-13 | イエール ユニバーシティ | タンパク質分解のイミド系モジュレーターおよび使用方法 |
WO2019191112A1 (en) | 2018-03-26 | 2019-10-03 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
WO2019241271A1 (en) | 2018-06-13 | 2019-12-19 | Biotheryx, Inc. | Fused thiophene compounds |
EP3820573B1 (en) | 2018-07-10 | 2023-08-09 | Novartis AG | 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases |
AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
EP3880669A1 (en) | 2018-11-13 | 2021-09-22 | Biotheryx, Inc. | Substituted isoindolinones |
CN113271945A (zh) | 2018-12-20 | 2021-08-17 | 诺华股份有限公司 | 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案和药物组合 |
AU2020374957A1 (en) | 2019-10-30 | 2022-04-28 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of Helios and methods of use |
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