AR102536A1 - INDOLAMINE OXIDORREDUCTASE IMMUNOMODULATING AGENTS - Google Patents
INDOLAMINE OXIDORREDUCTASE IMMUNOMODULATING AGENTSInfo
- Publication number
- AR102536A1 AR102536A1 ARP150103581A ARP150103581A AR102536A1 AR 102536 A1 AR102536 A1 AR 102536A1 AR P150103581 A ARP150103581 A AR P150103581A AR P150103581 A ARP150103581 A AR P150103581A AR 102536 A1 AR102536 A1 AR 102536A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alkyl
- cr5r5
- independently
- ring
- Prior art date
Links
- TXQAZWIBPGKHOX-UHFFFAOYSA-N 1H-indol-3-amine Chemical compound C1=CC=C2C(N)=CNC2=C1 TXQAZWIBPGKHOX-UHFFFAOYSA-N 0.000 title 1
- 239000002955 immunomodulating agent Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 102000006639 indoleamine 2,3-dioxygenase Human genes 0.000 abstract 2
- 108020004201 indoleamine 2,3-dioxygenase Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 101100439662 Arabidopsis thaliana CHR5 gene Proteins 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 101100516554 Caenorhabditis elegans nhr-5 gene Proteins 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- -1 SO2CH3 Chemical group 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Compuestos que modulan la enzima oxidorreductasa indolamina 2,3-dioxigenasa y composiciones que contienen los compuestos. También el uso de tales compuestos y composiciones para el tratamiento y/o la prevención de una gama diversa de enfermedades, trastornos y condiciones, incluyendo trastornos relacionados con cáncer e inmunorrelacionados, que están mediados por indolamina 2,3-dioxigenasa. Reivindicación 1: Un compuesto que tiene la fórmula (1) o una de sus sales, hidratos o solvatos farmacéuticamente aceptables, en donde, el subíndice n es 1 ó 0; el subíndice p es 1 ó 0; el anillo designado como A es fenilo, heteroarilo de 5 ó 6 miembros, o cicloalquilo C₅₋₇; Z es O; B es N, C(OR⁵ᵃ), o C(R³ᵃ); cada X es, de modo independiente, NR⁵ᵃ, O, CHR⁵, C(O), o CH(OR⁵ᵃ); Q es N, C(CN), o CR⁶; D es un enlace, O, C(R⁵)₂, o NR⁵ᵃ; E es un heteroarilo bicíclico fusionado opcionalmente sustituido de 9 ó 10 miembros; R¹ y R² son, de modo independiente, hidrógeno, halógeno, haloalquilo C₁₋₄ opcionalmente sustituido, cicloalquilo C₃₋₆ opcionalmente sustituido, cicloheteroalquilo de 3 a 6 miembros opcionalmente sustituido, fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, alquilo C₁₋₄ opcionalmente sustituido, alcoxi C₁₋₄ opcionalmente sustituido, CN, SO₂NH₂, NHSO₂CH₃, NHSO₂CF₃, OCF₃, SO₂CH₃, SO₂CF₃, o CONH₂, y cuando R¹ y R² están en vértices adyacentes de un anillo fenilo se pueden unir para formar un anillo cicloheteroalquilo de 5 ó 6 miembros que tiene uno o dos vértices de anillo seleccionados, de modo independiente, de O, N y S, en donde dicho anillo cicloheteroalquilo está opcionalmente sustituido con uno a tres miembros seleccionados de fluoro y alquilo C₁₋₃; R³, R³ᵃ y R⁴ son, de modo independiente, hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, haloalquilo C₁₋₆ opcionalmente sustituido, cicloalquil C₃₋₆-alquilo C₁₋₄ opcionalmente sustituido, aril-alquilo C₁₋₆ opcionalmente sustituido, flúor, OH, CN, CO₂H, C(O)NH₂, N(R⁵)₂, -O-alquilo C₁₋₆ opcionalmente sustituido, -(CR⁵R⁵)ₘ-OH, -(CR⁵R⁵)ₘ-CO₂H, -(CR⁵R⁵)ₘ-C(O)NH₂, -(CR⁵R⁵)ₘ-C(O)NHR⁵, -(CR⁵R⁵)ₘN(R⁵)₂, -NH(CR⁵R⁵)ₘCO₂H o -NH(CR⁵R⁵)ₘ-C(O)NH₂; cada R⁵ es, de modo independiente, H, F, OH, o alquilo C₁₋₆ opcionalmente sustituido; cada R⁵ᵃ es, de modo independiente, H, o alquilo C₁₋₆ opcionalmente sustituido; R⁶ es H, OH, F, alquilo C₁₋₆ opcionalmente sustituido, -O-alquilo C₁₋₆ opcionalmente sustituido, o -N(R⁵ᵃ)₂; y cada m es, de modo independiente, 1, 2, ó 3.Compounds that modulate the enzyme oxidoreductase indolamine 2,3-dioxygenase and compositions containing the compounds. Also the use of such compounds and compositions for the treatment and / or prevention of a diverse range of diseases, disorders and conditions, including cancer-related and immune-related disorders, which are mediated by indolamine 2,3-dioxygenase. Claim 1: A compound having the formula (1) or a pharmaceutically acceptable salt, hydrate or solvate, wherein the subscript n is 1 or 0; the subscript p is 1 or 0; the ring designated as A is phenyl, 5- or 6-membered heteroaryl, or C₅₋₇ cycloalkyl; Z is O; B is N, C (OR⁵ᵃ), or C (R³ᵃ); each X is, independently, NR⁵ᵃ, O, CHR⁵, C (O), or CH (OR⁵ᵃ); Q is N, C (CN), or CR⁶; D is a bond, O, C (R⁵) ₂, or NR⁵ᵃ; E is an optionally substituted 9 or 10 membered fused bicyclic heteroaryl; R¹ and R² are independently hydrogen, halogen, optionally substituted C₁₋₄ haloalkyl, optionally substituted C₃₋₆ cycloalkyl, optionally substituted 3 to 6 membered cycloheteroalkyl, optionally substituted phenyl, optionally substituted heteroaryl, optionally substituted C₁₋₄ alkyl , optionally substituted C₁₋₄ alkoxy, CN, SO₂NH₂, NHSO₂CH₃, NHSO₂CF₃, OCF₃, SO₂CH₃, SO₂CF₃, or CONH₂, and when R¹ and R² are at adjacent vertices of a phenyl ring they can be joined to form a cycloheteroalkyl ring of 5 or 6 members having one or two ring vertices independently selected from O, N and S, wherein said cycloheteroalkyl ring is optionally substituted with one to three members selected from fluoro and C₁₋₃ alkyl; R³, R³ᵃ and R⁴ are, independently, hydrogen, optionally substituted C₁₋₆ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl-C alquilo alkyl optionally substituted, optionally substituted aryl-C₁₋₆ alkyl, fluorine, OH, CN, CO₂H, C (O) NH₂, N (R⁵) ₂, -O-optionally substituted C₁₋₆ alkyl, - (CR⁵R⁵) ₘ-OH, - (CR⁵R⁵) ₘ-CO₂H, - (CR⁵R⁵) ₘ-C (O) NH₂, - (CR⁵R⁵) ₘ-C (O) NHR⁵, - (CR⁵R⁵) ₘN (R⁵) ₂, -NH (CR⁵R⁵) ₘCO₂H or - NH (CR⁵R⁵) ₘ-C (O) NH₂; each R⁵ is, independently, H, F, OH, or optionally substituted C₁₋₆ alkyl; each R⁵ᵃ is, independently, H, or optionally substituted C₁₋₆ alkyl; R⁶ is H, OH, F, optionally substituted C₁₋₆ alkyl, -O-optionally substituted C₁₋₆ alkyl, or -N (R⁵ᵃ) ₂; and each m is, independently, 1, 2, or 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462075671P | 2014-11-05 | 2014-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102536A1 true AR102536A1 (en) | 2017-03-08 |
Family
ID=58688564
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150103581A AR102536A1 (en) | 2014-11-05 | 2015-11-04 | INDOLAMINE OXIDORREDUCTASE IMMUNOMODULATING AGENTS |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR102536A1 (en) |
| MA (2) | MA47036B1 (en) |
-
2015
- 2015-11-04 AR ARP150103581A patent/AR102536A1/en active IP Right Grant
- 2015-11-05 MA MA47036A patent/MA47036B1/en unknown
-
2017
- 2017-05-04 MA MA40289A patent/MA40289A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MA40289A1 (en) | 2018-01-31 |
| MA47036B1 (en) | 2020-11-30 |
| MA47036A1 (en) | 2020-05-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |