AR113959A1 - Compuestos de 4-azaindol - Google Patents
Compuestos de 4-azaindolInfo
- Publication number
- AR113959A1 AR113959A1 ARP180103685A ARP180103685A AR113959A1 AR 113959 A1 AR113959 A1 AR 113959A1 AR P180103685 A ARP180103685 A AR P180103685A AR P180103685 A ARP180103685 A AR P180103685A AR 113959 A1 AR113959 A1 AR 113959A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- crxrx
- nrx
- nrxrx
- hydroxyalkyl
- Prior art date
Links
- XWIYUCRMWCHYJR-UHFFFAOYSA-N 1h-pyrrolo[3,2-b]pyridine Chemical class C1=CC=C2NC=CC2=N1 XWIYUCRMWCHYJR-UHFFFAOYSA-N 0.000 title 1
- -1 heptanyl Chemical group 0.000 abstract 93
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 29
- 125000000217 alkyl group Chemical group 0.000 abstract 23
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 22
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 20
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 19
- 125000003386 piperidinyl group Chemical group 0.000 abstract 19
- 125000004076 pyridyl group Chemical group 0.000 abstract 17
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 15
- 125000002757 morpholinyl group Chemical group 0.000 abstract 15
- 125000004193 piperazinyl group Chemical group 0.000 abstract 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 13
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 11
- 125000001424 substituent group Chemical group 0.000 abstract 11
- 125000002393 azetidinyl group Chemical group 0.000 abstract 10
- 150000001875 compounds Chemical class 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 8
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 8
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 8
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 8
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 7
- 125000005959 diazepanyl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000002883 imidazolyl group Chemical group 0.000 abstract 5
- 125000003566 oxetanyl group Chemical group 0.000 abstract 5
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 abstract 5
- 125000001425 triazolyl group Chemical group 0.000 abstract 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- 125000003725 azepanyl group Chemical group 0.000 abstract 3
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 3
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 3
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 abstract 3
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 3
- 125000000335 thiazolyl group Chemical group 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 2
- 125000002541 furyl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 125000003944 tolyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- WRYCSMQKUKOKBP-UHFFFAOYSA-N Imidazolidine Chemical compound C1CNCN1 WRYCSMQKUKOKBP-UHFFFAOYSA-N 0.000 abstract 1
- 102000002689 Toll-like receptor Human genes 0.000 abstract 1
- 108020000411 Toll-like receptor Proteins 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000005605 benzo group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000005879 dioxolanyl group Chemical group 0.000 abstract 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 abstract 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000001984 thiazolidinyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos de fórmula (1), N-óxidos, o sus sales, donde G, A, R¹, R⁵, y n se definen en la presente. También métodos de uso de tales compuestos como inhibidores de señalización a través del receptor tipo Toll 7, o 8, o 9, y composiciones farmacéuticas que comprenden tales compuestos. Estos compuestos son útiles para tratar enfermedades inflamatorias y autoinmunes. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), N-óxido, o una de sus sales, donde: G es: (i) un compuesto de fórmula (2); (ii) un compuesto del grupo de fórmulas (3); (iii) un compuesto del grupo de fórmulas (4); (iv) un anillo heterocíclico de 9 miembros seleccionado de los compuestos del grupo de fórmulas (5); o (v) anillo heterocíclico de 10 miembros seleccionado de los compuestos del grupo de fórmulas (6); A es: (i) -O-L¹-R⁶; (ii) -NR⁷R⁸; (iii) -L²-C(O)NR⁹R¹⁰; (iv) -(CRˣRˣ)₁₋₃R¹¹, aminoalquilo C₁₋₃, -(CRˣRˣ)₁₋₃NRˣC(O)R¹¹, -(CRˣRˣ)₁₋₂NRˣC(O)(CH₂)₁₋₂(piperidinilo), -(CRˣRˣ)₁₋₂NRˣC(O)O(CH₂)₁₋₂(piperidinilo), o -(CRˣRˣ)₁₋₂NRˣC(O)(CH₂)₁₋₂NRˣRˣ; (v) -CRˣR¹²R¹³, donde R¹² y R¹³ junto con el átomo de carbono al que están unidos forman un grupo cíclico seleccionado de azabiciclo[4,1,1]octanilo, azepanilo, azetidinilo, cicloalquilo C₃₋₇, diazepanilo, azaspiro[3,3]heptanilo, diazaspiro[4,5]decanonilo, morfolinilo, octahidrociclopenta[c]pirrolilo, piperazinilo, piperidinilo, pirrolidinilo, y quinuclidinilo, cada uno sustituido con cero a 4 R¹²ᵃ; (vi) -CRˣ=CRˣ(piperidinilo); o (vii) un grupo aromático seleccionado de [1,2,4]triazol[1,5-a]piridinilo, imidazo[1,2-a]piridinilo, imidazolilo, indazolilo, isoquinolinilo, oxadiazolilo, oxazolilo, fenilo, pirazinilo, pirazolo[3,4-b]piridinilo, pirazolilo, piridazinilo, piridinilo, pirimidinilo, pirrolilo, quinolinonilo, quinolinilo, quinoxalinilo, tetrahidro-[1,2,4]triazol[1,5-a]pirazinilo, tetrahidroimidazol[1,2-a]pirazinilo, tetrahidroisoquinolinilo, tetrahidrotiazolo[5,4-c]piridinilo, tetrahidrotieno[2,3-c]piridinilo, tiadiazolilo, tiazolilo, tiooxadiazolilo, y triazolilo, cada uno sustituido con cero a 2 R¹⁴ᵃ, y cero a 3 R¹⁴ᵇ; L¹ es un enlace, -(CRˣRˣ)₁₋₂-, -(CRˣRˣ)₁₋₂CRˣ(OH)-, -(CRˣRˣ)₁₋₂O-, -CRˣRˣC(O)-, -CRˣRˣC(O)NRˣ(CRˣRˣ)₀₋₄-, -CRˣRˣNRˣC(O)(CRˣRˣ)₀₋₄-, o -CRˣRˣNRˣC(O)(CRˣRˣ)₀₋₄-; L² es un enlace o -(CRˣRˣ)₁₋₃-; R¹ es H, Cl, -CN, alquilo C₁₋₄, fluoroalquilo C₁₋₃, hidroxialquilo C₁₋₃, hidroxi-fluoroalquilo C₁₋₃, -CRᵛ=CH₂, cicloalquilo C₃₋₆, -CH₂(cicloalquilo C₃₋₆), -C(O)O(alquilo C₁₋₃), o tetrahidropiranilo; cada R² es de modo independiente halo, -CN, -OH, -NO₂, alquilo C₁₋₄, fluoroalquilo C₁₋₂, cianoalquilo C₁₋₂, hidroxialquilo C₁₋₃, aminoalquilo C₁₋₃, -O(CH₂)₁₋₂OH, -(CH₂)₀₋₄O(alquilo C₁₋₄), fluoroalcoxi C₁₋₃, -(CH₂)₁₋₄O(alquilo C₁₋₃), -O(CH₂)₁₋₂OC(O)(alquilo C₁₋₃), -O(CH₂)₁₋₂NRˣRˣ, -C(O)O(alquilo C₁₋₃), -(CH₂)₀₋₂C₍O₎NRʸRʸ, -C(O)NRˣ(hidroxialquilo C₁₋₅), -C(O)NRˣ(alcoxialquilo C₂₋₆), -C(O)NRˣ(cicloalquilo C₃₋₆), -NRʸRʸ, -NRʸ(fluoroalquilo C₁₋₃), -NRʸ(hidroxialquilo C₁₋₄), -NRˣCH₂(fenilo), -NRˣS(O)₂(cicloalquilo C₃₋₆), -NRˣC(O)(alquilo C₁₋₃), -NRˣCH₂(cicloalquilo C₃₋₆), -(CH₂)₀₋₂S(O)₂(alquilo C₁₋₃), -(CH₂)₀₋₂(cicloalquilo C₃₋₆), -(CH₂)₀₋₂(fenilo), morfolinilo, dioxotiomorfolinilo, dimetil pirazolilo, metilpiperidinilo, metilpiperazinilo, amino-oxadiazolilo, imidazolilo, triazolilo, o -C(O)(tiazolilo); R²ᵃ es alquilo C₁₋₆, fluoroalquilo C₁₋₃, hidroxialquilo C₁₋₆, aminoalquilo C₁₋₃, -(CH₂)₀₋₄O(alquilo C₁₋₃), cicloalquilo C₃₋₆, -(CH₂)₁₋₃C₍O₎NRˣRˣ, -CH₂(cicloalquilo C₃₋₆), -CH₂(fenilo), tetrahidrofuranilo, tetrahidropiranilo, o fenilo; cada R²ᵇ es de modo independiente H, halo, -CN, -NRˣRˣ, alquilo C₁₋₆, fluoroalquilo C₁₋₃, hidroxialquilo C₁₋₃, fluoroalcoxi C₁₋₃, -(CH₂)₀₋₂O(alquilo C₁₋₃), -(CH₂)₀₋₃C₍O₎NRˣRˣ, -(CH₂)₁₋₃(cicloalquilo C₃₋₆), -C(O)O(alquilo C₁₋₃), -C(O)NRˣ(alquilo C₁₋₃), -CRˣ=CRˣRˣ, o -CRˣ=CH(cicloalquilo C₃₋₆); R²ᶜ es R²ᵃ o R²ᵇ; R²ᵈ es R²ᵃ o R²ᵇ; con la condición de que uno de R²ᶜ y R²ᵈ es R²ᵃ, y el otro de R²ᶜ y R²ᵈ es R²ᵇ; cada R⁵ es de modo independiente F, Cl, -CN, alquilo C₁₋₃, fluoroalquilo C₁₋₂, o -OCH₃; R⁶ es: (i) alquilo C₁₋₃, -CRˣRˣC(O)NRˣ(CRˣRˣ)₁₋₃OH, -CRˣRˣC(O)NRˣ(CRˣRˣ)₁₋₂NRˣRˣ, o -CRˣRˣC(O)NRˣ(CRˣRˣ)₁₋₂CHFCRˣRˣOH; o (ii) azabiciclo[3,2,1]octanilo, azaspiro[5,5]undecanilo, azetidinilo, cicloalquilo C₃₋₆, diazabiciclo[2,2,1]heptanilo, diazaspiro[3,5]nonanilo, morfolinilo, tetrahidrofuranilo, tetrahidropiranilo, octahidrociclopenta[c]pirrolilo, piperazinilo, piperidinilo, pirrolidinilo, o quinuclidinilo, cada uno sustituido con cero a 3 R⁶ᵃ; cada R⁶ᵃ es de modo independiente F, Cl, -OH, -CN, alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₆, -(CH₂)₁₋₂O(alquilo C₁₋₃), -NRʸRʸ, -(CH₂)₁₋₂NRˣRˣ, -(CRˣRˣ)₁₋₂S(O)₂(alquilo C₁₋₃), -(CRˣRˣ)₁₋₂C₍O₎NRˣRˣ, -C(O)(CRˣRˣ)₁₋₂NRˣRˣ, oxetanilo, tetrahidrofuranilo, tetrahidropiranilo, azetidinilo, pirrolidinilo, piperidinilo, isobutilpiperidinilo, piperazinilo, o -O(piperidinilo); R⁷ es: (i) R⁷ᵃ, -CH₂R⁷ᵃ, -(CH₂)₁₋₃NRʸRʸ, -(CH₂)₁₋₃NRˣC(O)(CH₂)₁₋₂NRʸRʸ, -C(O)R⁷ᵃ, -C(O)CH(NH₂)R⁷ᵃ, -C(O)(CH₂)₁₋₃NH₂, -C(O)CH(NH₂)(alquilo C₁₋₄), -C(O)CH(NH₂)(CH₂)₁₋₂C₍O₎OH, ₋C₍O₎CH₍NH₂)(CH₂)₂₋₄NH₂, o -C(O)CH(NH₂)(CH₂)₁₋₃C₍O₎NH₂; o (ii) cicloalquilo C₃₋₆ sustituido con un sustituyente seleccionado de -NRˣ(CH₂)₂₋₃NRʸRʸ, -NRˣ(metilpiperidinilo), -NRˣ(CH₂)₂₋₃(morfolinilo), dimetilamino piperidinilo, y piperazinilo sustituido con un sustituyente seleccionado de alquilo C₁₋₄, -C(O)CH₃, -(CH₂)₁₋₂OCH₃, -CH₂(metilfenilo), -(CH₂)₂₋₃(pirrolidinilo), cicloalquilo C₃₋₆, piridinilo, y metilpiperidinilo; R⁷ᵃ es azaspiro[3,5]nonanilo, cicloalquilo C₃₋₆, diazaspiro[3,5]nonanilo, diazaspiro[5,5]undecanilo, diazepanonilo, diazepanilo, morfolinilo, fenilo, piperazinilo, piperidinilo, pirrolidinonilo, pirrolidinilo, o pirrolilo, cada uno sustituido con cero a 1 sustituyente seleccionado de alquilo C₁₋₃, -NH₂, metilpiperidinilo, metilpirrolidinilo, -OCH₂CH₂(pirrolidinilo), y -OCH₂CH₂NHCH₂CH₃; y cero a 4 sustituyentes seleccionados de -CH₃; R⁷ᵇ es: (i) -OH, alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, aminoalquilo C₁₋₃, -(CH₂)₂₋₃CºCH, -(CRˣRˣ)₁₋₂O(alquilo C₁₋₂), -(CH₂)₁₋₃S(O)₂(alquilo C₁₋₂), -(CH₂)₀₋₃NRˣRʸ, -(CH₂)₁₋₂C₍O₎NRˣRˣ, -NRʸRʸ, -NRˣ(hidroxialquilo C₁₋₄), -NRʸ(cianoalquilo C₁₋₂), -N(cianoalquilo C₁₋₂)₂, -NRˣ(fluoroalquilo C₁₋₄), -NRˣ(hidroxifluoroalquilo C₂₋₄), -(CRˣRˣ)₁₋₂C₍O₎NRˣRˣ, -NRˣ(CH₂)₁₋₂C₍O₎NRˣRˣ, -N((CH₂)₁₋₂C₍O₎NRˣRˣ)₂, -NRˣ(CH₂)₁₋₂S(O)₂(alquilo C₁₋₂), -NRˣ(CH₂)₁₋₃NRˣRˣ, -NRˣCH₂CH₂NRˣRˣ, -NRˣC(O)(CH₂)₁₋₂NRˣRˣ, -NRˣ(CH₂CH₂S(O)₂CH₃), (CH₂)₁₋₂NRˣC(O)(CH₂)₁₋₂NRˣRˣ, -O(CH₂)₁₋₃NRˣRˣ, -C(O)(CRˣRˣ)₁₋₂NRʸRʸ, -C(O)(CRˣRˣ)₁₋₂NRʸ(hidroxialquilo C₁₋₄), -C(O)(CRˣRˣ)₁₋₂NRˣ(CH₂CH₂OCH₃), -S(O)₂CH₂CH₂N(CH₃)₂, -(CH₂)₁₋₂R⁷ᵈ, -NRˣR⁷ᵈ, -NRˣ(CH₂)₁₋₂R⁷ᵈ, -NR⁷ᵈR⁷ᵈ, -N((CH₂)₁₋₂R⁷ᵈ)₂, -OR⁷ᵈ, -C(O)R⁷ᵈ, -C(O)(CRˣRˣ)₁₋₂R⁷ᵈ, o -C(O)(CRˣRˣ)₁₋₂NRˣR⁷ᵈ; o (ii) azepanilo, azetidinilo, cicloalquilo C₃₋₆, diazepanilo, dioxotetrahidrotiopiranilo, dioxotiomorfolinilo, morfolinilo, oxaazaspiro[3,3]heptanilo, oxaazaspiro[4,3]octanilo, oxetanilo, piperazinonilo, piperazinilo, piperidinilo, piridinilo, pirimidinilo, pirrolidinonilo, pirrolidinilo, tetrahidrofuranilo, tetrahidroisoquinolinilo, tetrahidropiranilo, o tiadiazolilo, cada uno sustituido con cero a 1 R⁸ᵃ y cero a 3 R⁸ᵇ; cada R⁷ᶜ es de modo independiente F, Cl, -CN, alquilo C₁₋₂, -CF₃, o -CH₂CN; R⁷ᵈ es azaspiro[3,5]nonanilo, azetidinilo, biciclo[1,1,1]pentanilo, cicloalquilo C₃₋₆, dioxotiaazaspiro[3,3]heptanilo, morfolinilo, oxaazaspiro[3,3]heptanilo, oxaazaspiro[4,3]octanilo, oxaazaspiro[4,4]nonilo, oxetanilo, fenilo, piperidinilo, pirazolilo, pirrolidinilo, tetrahidrofuranilo, tetrahidropiranilo, tiadiazolilo, o triazolilo, cada uno sustituido con cero a 2 sustituyentes seleccionados de modo independiente de F, -OH, alquilo C₁₋₃, hidroxialquilo C₁₋₂, alcoxi C₁₋₂, -NRˣRˣ, -C(O)CH₃, -S(O)₂CH₃, metilpiperidinilo, metilpirrolidinilo, tetrametilpiperidinilo, -OCH₂CH₂(pirrolidinilo), y -OCH₂CH₂NHCH₂CH₃; y cero a 4 sustituyentes seleccionados de -CH₃; R⁸ es H o alquilo C₁₋₃; o R⁷ y R⁸ junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico seleccionado de azetidinilo, diazabiciclo[2,2,1]heptanilo, diazabiciclo[2,2,2]octanilo, diazabiciclo[3,1,1]heptanilo, diazabiciclo[3,2,1]octanilo, azaspiro[3,3]heptanilo, diazaspiro[2,5]octanilo, diazaspiro[3,3]heptanilo, diazepanonilo, diazepanilo, diazaspiro[3,5]nonanilo, diazaspiro[5,5]undecanilo, imidazolilo, imidazolidinonilo, octahidro-1H-pirrol[3,4-b]piridinilo, oxadiazabiciclo[3,3,1]nonanilo, piperazinilo, piperazinonilo, piperidinilo, pirrolidinonilo, pirrolidinilo, y pirrolilo, donde dicho anillo heterocíclico está sustituido con cero a 1 R⁷ᵇ, y cero a 2 R⁷ᶜ; R⁸ᵃ es -OH, alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, -(CH₂)₁₋₂O(alquilo C₁₋₃), alcoxi C₁₋₂, -C(O)(alquilo C₁₋₃), -C(O)O(alquilo C₁₋₂), -(CH₂)₁₋₂(cicloalquilo C₃₋₆), -(CH₂)₁₋₃(metilfenilo), -(CH₂)₁₋₃(pirrolidinilo), -(CH₂)₁₋₃(metilpirazolilo), -(CH₂)₁₋₃(tiofenilo), -NRˣRˣ, cicloalquilo C₃₋₆, metilpiperidinilo, piridinilo, o pirimidinilo; cada R⁸ᵇ, es de modo independiente F, Cl, -CN, alquilo C₁₋₃, o -CF₃; R⁹ es alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₆, hidroxi fluoroalquilo C₁₋₆, aminoalquilo C₁₋₃, -(CH₂)₁₋₂O(alquilo C₁₋₃), -(CH₂)₁₋₃NRˣRˣ, -(CH₂)₁₋₂C₍O₎NRˣRˣ, -(CH₂)₁₋₃S(O)₂OH, -(CRˣRˣ)₁₋₃NRˣS(O)₂(alquilo C₁₋₂), o -(CH₂)₀₋₃R⁹ᵃ; R⁹ᵃ es cicloalquilo C₃₋₇, furanilo, fenilo, piperazinilo, piperidinilo, pirazolilo, piridinilo, pirrolidinilo, quinuclidinilo, tiazolilo, o octahidrociclopenta[c]pirrolilo, cada uno sustituido con cero a 3 sustituyentes seleccionados de modo independiente de F, Cl, -OH, alquilo C₁₋₄, hidroxialquilo C₁₋₃, hidroxi fluoroalquilo C₁₋₃, aminoalquilo C₁₋₃, -NRʸRʸ, oxetanilo, fenilo, piperazinilo, piperidinilo, y pirrolidinilo; R¹⁰ es H, alquilo C₁₋₄, -(CH₂)₁₋₃O(alquilo C₁₋₄), o cicloalquilo C₃₋₆; o R⁹ y R¹⁰ junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico seleccionado de azabiciclo[3,1,1]heptanilo, azaspiro[5,5]undecanilo, diazabiciclo[2,2,1]heptanilo, diazabiciclo[3,1,1]heptanilo, diazabiciclo[3,2,0]heptanilo, diazaspiro[3,5]nonanilo, diazaspiro[4,4]nonanilo, diazaspiro[4,5]decanilo, diazepanilo, indolinilo, morfolinilo, octahidropirrol[3,4-c]pirrolilo, piperazinonilo, piperazinilo, piperidinilo, y pirrolidinilo, cada uno sustituido con cero a 3 R¹⁰ᵃ; cada R¹⁰ᵃ es de modo independiente alquilo C₁₋₄, hidroxialquilo C₁₋₄, -(CH₂)₁₋₃O(alquilo C₁₋₃), -(CH₂)₁₋₃NRˣRˣ, -(CH₂)₁₋₂C₍O₎NRˣRˣ, -(CH₂)₁₋₂(metiltriazolilo), -CH₂CH₂(fenilo), -CH₂CH₂(morfolinilo), -C(O)(alquilo C₁₋₂), -C(O)NRʸRʸ, -C(O)CH₂NRʸRʸ, -NRʸRʸ, -NHC(O)(alquilo C₁₋₃), -C(O)(furanilo), -O(piperidinilo), -C(O)CH₂(dietilcarbamoilpiperidinilo), metilpiperazinilo, piperidinilo, metilpiperidinilo, dietilcarbamoilpiperidinilo, isopropilpiperidinilo, piridinilo, trifluorometilpiridinilo, pirimidinilo, o dihidrobenzo[d]imidazolonilo; R¹¹ es azetidinilo, azaspiro[3,5]nonanilo, dioxidotiomorfolinilo, hexahidropirrol[3,4-c]pirrolilo, morfolinilo, piperazinilo, piperidinilo, piridinilo, o pirrolidinilo, cada uno sustituido con cero a 3 sustituyentes seleccionados de modo independiente de halo, -CN, alquilo C₁₋₄, aminoalquilo C₁₋₃, -(CH₂)₁₋₂(metiloxetanilo), -(CH₂)₁₋₂(triazolilo), -(CH₂)₁₋₂(fenilo), -C(O)CH₂NRˣRˣ, hidroxialquilo C₁₋₅, -(CH₂)₁₋₂C₍O₎NRˣRˣ, -(CH₂)₁₋₂S(O)₂(alquilo C₁₋₃), -(CH₂)₁₋₂S(O)(alquilo C₁₋₃), oxetanilo, tetrahidrofuranilo, y tetrahidropiranilo; cada R¹²ᵃ es de modo independiente F, Cl, -OH, alquilo C₁₋₆, fluoroalquilo C₁₋₄, cianoalquilo C₁₋₄, hidroxialquilo C₁₋₆, -(CH₂)₁₋₂O(alquilo C₁₋₄), -(CH₂)₁₋₂C₍O₎NRˣRˣ, -(CH₂)₁₋₂S(O)₂(alquilo C₁₋₂), -(CH₂)₁₋₂NRˣHS(O)₂(alquilo C₁₋₂), -(CH₂)₁₋₂NRˣRˣ, alcoxi C₁₋₃, -NRʸRʸ, -NRˣ(fluoroalquilo C₁₋₄), -NRˣ(cianoalquilo C₁₋₂), -NRˣCH₂NRˣRˣ, -NRˣ(hidroxialquilo C₁₋₄), -NRˣ(CRˣRˣCRˣRˣ)O(alquilo C₁₋₃), -NRˣ(CH₂C(O)NRˣRˣ), -NRˣ(alcoxi C₁₋₃), -NRˣCH₂CH₂S(O)₂(alquilo C₁₋₂), -NRˣC(O)CH₃, -NRˣC(O)(fluoroalquilo C₁₋₂), -NRˣC(O)CRˣRˣNRˣRˣ, -NRˣC(O)CH₂NRʸRʸ, -NRˣC(O)CH₂NRˣ(hidroxialquilo C₁₋₄), -NRˣ(CH₂)₁₋₂C₍O₎NRˣRˣ, -NRˣS(O)₂(alquilo C₁₋₂), -C(O)(alquilo C₁₋₅), -C(O)(CH₂)₁₋₃O(alquilo C₁₋₂), -C(O)(CRˣRˣ)₁₋₂NRʸRʸ, R¹²ᵇ, -CRˣRˣR¹²ᵇ, -C(O)R¹²ᵇ, -C(O)CRˣRˣNRˣR¹²ᵇ, -C(O)NRˣR¹²ᵇ, -NRˣC(O)CRˣRˣR¹²ᵇ, -NRˣR¹²ᵇ, -NRˣCRˣRˣR¹²ᵇ, -N(CH₂CN)R¹²ᵇ, -NRˣC(O)CRˣRˣNRˣR¹²ᵇ, -NRˣC(O)CRˣRˣNRˣCH₂R¹²ᵇ, -NRˣCRˣRˣC(O)NRˣR¹²ᵇ, o -OR¹²ᵇ; o dos R¹²ᵃ y el átomo de carbono al cual están unidos forman C=O; R¹²ᵇ es azetidinilo, biciclo[1,1,1]pentanilo, cicloalquilo C₃₋₆, diazabiciclo[2,2,1]heptanilo, dioxolanilo, dioxotiaazaspiro[3,3]heptanilo, dioxidotetrahidrotiopiranilo, dioxidotiomorfolinilo, imidazolilo, morfolinilo, octahidrociclopenta[c]pirrolilo, octahidropirrol[3,4-c]pirrolilo, oxaazaspiro[3,3]heptanilo, oxaazaspiro[4,3]octanilo, oxaazaspiro[4,4]nonanilo, oxetanilo, fenilo, piperazinilo, piperazinonilo, piperidinilo, piridinilo, pirrolidinilo, quinuclidinilo, tetrahidrofuranilo, tetrahidropiranilo, o triazolilo, cada uno sustituido con cero a 4 sustituyentes seleccionados de modo independiente de F, Cl, -OH, alquilo C₁₋₄, fluoroalquilo C₁₋₃, hidroxialquilo C₁₋₃, aminoalquilo C₁₋₃, alcoxi C₁₋₄, -(CH₂)₁₋₂O(alquilo C₁₋₃), -NRˣRˣ, -C(O)NRˣRˣ, y -CRˣRˣS(O)₂(alquilo C₁₋₃); cada R¹⁴ᵃ es de modo independiente es: (i) H, halo, -OH, alquilo C₁₋₆, fluoroalquilo C₁₋₂₃, hidroxialquilo C₁₋₄, -(CH₂)₁₋₂O(alquilo C₁₋₃), -CRˣRˣNRʸRʸ, -CRˣRˣNRˣ(C₁₋₃ cianoalquilo), -CRˣRˣNRˣ((CH₂)₁₋₂O(alquilo C₁₋₂)), -CRˣRˣN((CH₂)₁₋₂OCH₃)₂, -CRˣRˣNRˣ(CH₂CºCRˣ), -CRˣRˣNRˣ(CH₂)₁₋₃NRˣRˣ, -(CRˣRˣ)₁₋₃CRˣRˣNRˣRˣ, -CRˣ(NH₂)(CH₂)₁₋₄NRˣRˣ, -CRˣRˣNRˣ(CH₂)₁₋₂O(alquilo C₁₋₃), -CRˣRˣNRˣ(CH₂)₁₋₂O(CH₂)₁₋₂OH, -CRˣRˣNRˣ(CH₂)₁₋₃S(O)₂OH, -CRˣRˣC(O)NRˣRˣ, -NRˣRʸ, -NRˣ(CH₂)₁₋₃NRˣRˣ, -NRˣC(O)(alquilo C₁₋₃), -NRˣC(O)(fluoroalquilo C₁₋₃), -NRˣC(O)O(alquilo C₁₋₃), -NRˣC(O)(CH₂)₁₋₃NRˣRˣ, -NRˣCH₂C(O)CH₂NRˣRˣ, -C(O)(alquilo C₁₋₃), -C(O)(CRˣRˣ)₁₋₃OH, -C(O)CRˣRˣNRˣRˣ, -C(O)NRˣRˣ, -C(O)NRˣ(cianoalquilo C₁₋₂), -C(O)NRˣ(CRˣRˣ)₁₋₃NRˣRˣ, -C(O)N(CH₂CH₃)(CRˣRˣ)₁₋₃NRˣRˣ, -C(O)NRˣ(CRˣRˣ)₁₋₂C₍O₎NRˣRˣ, -C(O)NRˣ(CRˣRˣ)₁₋₃NRˣC(O)(alquilo C₁₋₂), -O(CRˣRˣ)₁₋₃NRˣRˣ, -S(O)₂NRˣRˣ, o -C(O)(CRˣRˣ)₁₋₂S(O)₂(alquilo C₁₋₂); (ii) 8-azabiciclo[3,2,1]octanilo, azaspiro[3,5]nonanilo, azetidinilo, benzo[c][1,2,5]oxadiazolilo, ciclopentilo, ciclohexilo, diazepanilo, morfolinilo, fenilo, piperazinilo, piperidinilo, pirazolilo, piridinilo, pirrolidinonilo, quinolinilo, quinuclidinilo, tetrahidroisoquinolinilo, tetrahidropiridinilo, o tiazolidinilo, cada uno sustituido con cero a 2 sustituyentes seleccionados de modo independiente de alquilo C₁₋₄, fluoroalquilo C₁₋₂, hidroxialquilo C₁₋₄, -NRˣRˣ, -(CH₂)₁₋₂NRˣRˣ, -C(O)(alquilo C₁₋₂), -C(O)CH₂NRˣRˣ, -C(O)O(alquilo C₁₋₃), -CH₂C(O)NRˣRˣ, cicloalquilo C₃₋₆, -CH₂(fenilo), -CH₂(pirrolilo), -CH₂(morfolinilo), -CH₂(metilpiperazinilo), -CH₂(tiofenilo), metilpiperidinilo, isobutilpiperidinilo, y piridinilo; o (iii) -L³-R¹⁴ᶜ; cada R¹⁴ᵇ, es F, Cl, -OH, -CH₃, o -OCH₃; R¹⁴ᶜ es adamantanilo, azepanilo, azetidinilo, cicloalquilo C₃₋₇, diazepanilo, imidazolilo, indolilo, morfolinilo, octahidropirrol[3,4-c]pirrolilo, fenilo, piperazinonilo, piperazinilo, piperidinilo, piridinilo, pirrolidinonilo, pirrolidinilo, pirrolilo, triazolilo, o tetrazolilo, cada uno sustituido con cero a 1 sustituyente seleccionado de F, -OH, alquilo C₁₋₄, hidroxialquilo C₁₋₃, -NRˣRʸ, -NRˣC(O)CH₃, -C(O)(alquilo C₁₋₂), -C(O)NRˣRˣ, -C(O)N(CH₂CH₃)₂, -C(O)(tetrahidrofuranilo), -C(O)O(alquilo C₁₋₄), -CH₂C(O)NRˣRˣ, morfolinilo, metilpiperidinilo, pirazinilo, piridinilo, y pirrolidinilo; L3 es -(CRˣRˣ)₁₋₃-, -CH(NH₂)-, -CRˣRˣNRˣ, -C(O)-, -C(O)NRˣ(CH₂)₀₋₄-, -NRˣ-, -NRˣC(O)-, -NRˣCH₂-, -NRˣCH₂C(O)-, o -O(CH₂)₀₋₂-; Rᵛ es H, alquilo C₁₋₂, o fluoroalquilo C₁₋₂; cada Rˣ es de modo independiente H o -CH₃; cada Rʸ es de modo independiente H o alquilo C₁₋₆; n es cero, 1, ó 2; y p es cero, 1, 2, 3, ó 4.
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Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10071079B2 (en) | 2016-06-29 | 2018-09-11 | Bristol-Myers Squibb Company | [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds |
| MX2020006168A (es) * | 2017-12-18 | 2020-08-13 | Bristol Myers Squibb Co | Compuestos de 4-azaindol. |
| MX2020005622A (es) * | 2017-12-20 | 2020-08-20 | Bristol Myers Squibb Co | Compuestos de indol sustituidos con arilo y heteroarilo. |
| EA202091480A1 (ru) * | 2017-12-20 | 2020-11-06 | Бристол-Маерс Сквибб Компани | Аминоиндольные соединения, пригодные в качестве ингибиторов tlr |
| SG11202005733QA (en) * | 2017-12-20 | 2020-07-29 | Bristol Myers Squibb Co | Diazaindole compounds |
| EP3752505B1 (en) | 2018-02-12 | 2023-01-11 | F. Hoffmann-La Roche AG | Novel sulfone compounds and derivatives for the treatment and prophylaxis of virus infection |
| JP7434186B2 (ja) | 2018-06-12 | 2024-02-20 | エフ． ホフマン－ラ ロシュ アーゲー | 自己免疫疾患の処置のための新規のヘテロアリールヘテロシクリル化合物 |
| JP7366994B2 (ja) | 2018-07-23 | 2023-10-23 | エフ． ホフマン－ラ ロシュ アーゲー | 自己免疫疾患治療用の新規ピペラジン化合物 |
| JP7233809B2 (ja) | 2018-09-04 | 2023-03-07 | エフ． ホフマン－ラ ロシュ アーゲー | 自己免疫疾患の処置のためのベンゾチアゾール化合物 |
| JP2022502353A (ja) | 2018-09-06 | 2022-01-11 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 自己免疫疾患の処置のための新規の環状アミジン化合物 |
| JP2022550203A (ja) * | 2019-10-01 | 2022-11-30 | ブリストル－マイヤーズ スクイブ カンパニー | 置換二環ヘテロアリール化合物 |
| WO2021087181A1 (en) * | 2019-11-01 | 2021-05-06 | Bristol-Myers Squibb Company | Substituted pyrazole compounds as toll receptor inhibitors |
| IL300696A (en) * | 2020-08-19 | 2023-04-01 | Bristol Myers Squibb Co | ALTERNATIVE HETEROARYL COMPOUNDS ARE USEFUL AS TLR9 INHIBITORS |
| AU2021385752A1 (en) * | 2020-11-26 | 2023-06-29 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Fused tricyclic compound, preparation method therefor and application thereof in medicine |
| MX2023012110A (es) | 2021-04-16 | 2023-10-24 | Gilead Sciences Inc | Compuestos de tienopirrol. |
| CN117957234A (zh) | 2021-09-10 | 2024-04-30 | 吉利德科学公司 | 噻吩并吡咯化合物 |
| CN114591339B (zh) * | 2022-05-10 | 2022-08-02 | 上海维申医药有限公司 | 一类Toll样受体抑制剂及其制备和应用 |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100378937B1 (ko) | 1997-10-20 | 2003-05-09 | 에프. 호프만-라 로슈 아게 | 바이사이클릭 키나아제 억제제 |
| US6867200B1 (en) | 1998-12-18 | 2005-03-15 | Axys Pharmaceuticals, Inc. | (Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors |
| MXPA05013922A (es) | 2003-06-20 | 2006-02-24 | Coley Pharm Group Inc | Antagonistas de receptor tipo toll de molecula pequena. |
| WO2005111042A1 (en) | 2004-05-03 | 2005-11-24 | Janssen Pharmaceutica N.V. | Novel indole derivatives as selective androgen receptor modulators (sarms) |
| WO2007115306A2 (en) | 2006-04-04 | 2007-10-11 | Myriad Genetics, Inc. | Compounds for diseases and disorders |
| WO2006113458A1 (en) | 2005-04-15 | 2006-10-26 | Bristol-Myers Squibb Company | Heterocyclic inhibitors of protein arginine methyl transferases |
| DE102006033109A1 (de) | 2006-07-18 | 2008-01-31 | Grünenthal GmbH | Substituierte Heteroaryl-Derivate |
| US8027888B2 (en) | 2006-08-31 | 2011-09-27 | Experian Interactive Innovation Center, Llc | Online credit card prescreen systems and methods |
| WO2008065198A1 (en) | 2006-12-01 | 2008-06-05 | Galapagos N.V. | Triazolopyridine compounds useful for the treatment of degenerative & inflammatory diseases |
| GB0708141D0 (en) | 2007-04-26 | 2007-06-06 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
| WO2008152471A1 (en) | 2007-06-12 | 2008-12-18 | Coley Pharmaceutical Group, Inc. | Quinazoline derivative useful as toll-like receptor antagonist |
| WO2009030996A1 (en) | 2007-09-05 | 2009-03-12 | Coley Pharmaceutical Group, Inc. | Triazole compounds as toll-like receptor (tlr) agonists |
| CL2009000904A1 (es) * | 2008-04-21 | 2010-04-30 | Shionogi & Co | Compuestos derivados de ciclohexil sulfonamidas que tienen actividad antagonista en el receptor npy y5, composicion farmaceutica y formulacion farmaceutica que los comprende. |
| MX2011000216A (es) * | 2008-07-08 | 2011-03-29 | Intellikine Inc | Inhibidores de cinasa y metodos para su uso. |
| WO2010036905A1 (en) | 2008-09-26 | 2010-04-01 | Eisai R & D Management Co., Ltd. | Benzoxazole compounds and methods of use |
| WO2010045188A1 (en) | 2008-10-17 | 2010-04-22 | Boehringer Ingelheim International Gmbh | Heteroaryl substituted indole compounds useful as mmp-13 inhibitors |
| TW201639852A (zh) * | 2008-12-09 | 2016-11-16 | 吉李德科學股份有限公司 | 用於製備可用作類鐸受體調節劑之化合物的中間體化合物 |
| TWI462920B (zh) | 2009-06-26 | 2014-12-01 | 葛萊伯格有限公司 | 用於治療退化性及發炎疾病之新穎化合物 |
| CA2768236C (en) | 2009-07-16 | 2018-05-22 | Mallinckrodt Llc | (+)-morphinans as antagonists of toll-like receptor 9 and therapeutic uses thereof |
| WO2012054862A2 (en) | 2010-10-21 | 2012-04-26 | The Brigham And Women's Hospital, Inc. | Agents, compositions, and methods for treating pruritis and related skin conditions |
| PT2663550T (pt) | 2011-01-12 | 2017-03-22 | Array Biopharma Inc | Benzoazepinas substítuidas utilizáveis como moduladores dos recetores tipo toll |
| BR112013017947A2 (pt) | 2011-01-12 | 2018-12-18 | Array Biopharma Inc | benzoazepinas substituídas como moduladores de receptor toll-like |
| EP2713737B1 (en) | 2011-06-01 | 2016-04-20 | Janus Biotherapeutics, Inc. | Novel immune system modulators |
| JP6093759B2 (ja) | 2011-06-01 | 2017-03-08 | ジャナス バイオセラピューティクス，インク． | 新規の免疫系調節剤 |
| WO2012170867A1 (en) | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| AU2012285931B2 (en) | 2011-07-15 | 2017-01-12 | Cellzome Limited | Novel substituted indole derivatives as gamma secretase modulators |
| JP2013075834A (ja) | 2011-09-29 | 2013-04-25 | Kowa Co | Ｔｌｒ９阻害活性を有するピラゾロピリミジン−７−アミン誘導体 |
| IN2014KN00948A (es) | 2011-10-04 | 2015-08-21 | Janus Biotherapeutics Inc | |
| WO2013172479A1 (en) | 2012-05-18 | 2013-11-21 | Dainippon Sumitomo Pharma Co., Ltd. | Carboxylic acid compounds |
| JO3407B1 (ar) * | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| EP2738172A1 (en) | 2012-11-28 | 2014-06-04 | Almirall, S.A. | New bicyclic compounds as crac channel modulators |
| MA39034B1 (fr) | 2013-10-14 | 2018-09-28 | Eisai R&D Man Co Ltd | Composés de quinoline sélectivement substitués |
| EP3080124A1 (en) | 2013-12-13 | 2016-10-19 | Takeda Pharmaceutical Company Limited | Pyrrolo[3,2-c]pyridine derivatives as tlr inhibitors |
| EP3190113B1 (en) | 2014-08-15 | 2021-05-19 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Pyrrolopyrimidine compounds used as tlr7 agonist |
| US20170275287A1 (en) | 2014-08-22 | 2017-09-28 | Janus Biotherapeutics, Inc. | Novel n2, n4, n7, 6-tetrasubstituted pteridine-2,4,7-triamine and 2, 4, 6, 7-tetrasubstituted pteridine compounds and methods of synthesis and use thereof |
| TW201630907A (zh) | 2014-12-22 | 2016-09-01 | 必治妥美雅史谷比公司 | ＴＧＦβＲ拮抗劑 |
| SG11201900619XA (en) * | 2016-07-30 | 2019-02-27 | Bristol Myers Squibb Co | Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors |
| EP3510024B1 (en) * | 2016-09-09 | 2021-11-17 | Bristol-Myers Squibb Company | Pyridyl substituted indole compounds |
| MX2020006168A (es) * | 2017-12-18 | 2020-08-13 | Bristol Myers Squibb Co | Compuestos de 4-azaindol. |
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