AR124718A1 - Quinolinas y azaquinolinas como inhibidores de cd38 - Google Patents
Quinolinas y azaquinolinas como inhibidores de cd38Info
- Publication number
- AR124718A1 AR124718A1 ARP220100173A ARP220100173A AR124718A1 AR 124718 A1 AR124718 A1 AR 124718A1 AR P220100173 A ARP220100173 A AR P220100173A AR P220100173 A ARP220100173 A AR P220100173A AR 124718 A1 AR124718 A1 AR 124718A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- nrc3rd3
- membered
- nrc3c
- haloalkyl
- Prior art date
Links
- 102100031585 ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Human genes 0.000 title 1
- 101000777636 Homo sapiens ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Proteins 0.000 title 1
- 229940111121 antirheumatic drug quinolines Drugs 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003248 quinolines Chemical class 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 22
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 11
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 10
- 125000005843 halogen group Chemical group 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 9
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 abstract 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 4
- 101100310926 Caenorhabditis elegans sra-3 gene Proteins 0.000 abstract 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 2
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 2
- 101100150274 Caenorhabditis elegans srb-2 gene Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- -1 C2−6 alky nile Chemical group 0.000 abstract 1
- 102100038417 Cytoplasmic FMR1-interacting protein 1 Human genes 0.000 abstract 1
- 101710181791 Cytoplasmic FMR1-interacting protein 1 Proteins 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal farmacéuticamente aceptable del mismo, donde: X³ es CR³ o N; X⁴ es CR⁴ o N; A es un heteroarilo de 5 miembros que tiene 1, 2 ó 3 heteroátomos que forman parte del anillo seleccionados entre N, O, y S, donde el heteroarilo de 5 miembros de A está opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre halo y C₁₋₄ alquilo; L es un conector C₁₋₄ alquileno; n es 0 ó 1; Q es H, C₁₋₁₀ alquilo, C₂₋₁₀ alquenilo, C₂₋₁₀ alquinilo, C₁₋₁₀ haloalquilo, C₆₋₁₀ arilo, C₃₋₁₄ cicloalquilo, heteroarilo de 5 - 14 miembros, o heterocicloalquilo de 4 - 14 miembros, donde dichos C₁₋₁₀ alquilo, C₂₋₁₀ alquenilo, C₂₋₁₀ alquinilo, C₁₋₁₀ haloalquilo, C₆₋₁₀ arilo, C₃₋₁₄ cicloalquilo, heteroarilo de 5 - 14 miembros, y heterocicloalquilo de 4 - 14 miembros de Q están opcionalmente sustituidos en cada caso con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre Cy¹, Cy¹-C₁₋₄ alquilo, halo, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, CN, NO₂, ORᵃ, SRᵃ, C(O)Rᵇ, C(O)NRᶜRᵈ, C(O)ORᵃ, OC(O)Rᵇ, OC(O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(O)Rᵇ, NRᶜC(O)ORᵃ, NRᶜC(O)NRᶜRᵈ, NRᶜS(O)Rᵇ, NRᶜS(O)₂Rᵇ, NRᶜS(O)₂NRᶜRᵈ, S(O)Rᵇ, S(O)NRᶜRᵈ, S(O)₂Rᵇ, y S(O)₂NRᶜRᵈ, donde dichos C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre Cy¹, CN, NO₂, ORᵃ, SRᵃ, C(O)Rᵇ, C(O)NRᶜRᵈ, C(O)ORᵃ, OC(O)Rᵇ, OC(O)NRᶜRᵈ, C(=NRᵉ)NRᶜRᵈ, NRᶜC(=NRᵉ)NRᶜRᵈ, NRᶜRᵈ, NRᶜC(O)Rᵇ, NRᶜC(O)ORᵃ, NRᶜC(O)NRᶜRᵈ, NRᶜS(O)Rᵇ, NRᶜS(O)₂Rᵇ, NRᶜS(O)₂NRᶜRᵈ, S(O)Rᵇ, S(O)NRᶜRᵈ, S(O)₂Rᵇ, y S(O)₂NRᶜRᵈ; cada Cy¹ se selecciona en forma independiente entre C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 10 miembros, y heterocicloalquilo de 4 - 10 miembros, cada uno opcionalmente sustituido con 1, 2, 3, ó 4 sustituyentes seleccionados en forma independiente entre halo, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, C₆₋₁₀ aril-C₁₋₄ alquilo, C₃₋₇ cicloalquil-C₁₋₄ alquilo, heteroaril-C₁₋₄ alquilo de 5 - 10 miembros, heterocicloalquil-C₁₋₄ alquilo de 4 - 10 miembros, CN, NO₂, ORᵃ¹, SRᵃ¹, C(O)Rᵇ¹, C(O)NRᶜ¹Rᵈ¹, C(O)ORᵃ¹, OC(O)Rᵇ¹, OC(O)NRᶜ¹Rᵈ¹, C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C(O)Rᵇ¹, NRᶜ¹C(O)ORᵃ¹, NRᶜ¹C(O)NRᶜ¹Rᵈ¹, NRᶜ¹S(O)Rᵇ¹, NRᶜ¹S(O)₂Rᵇ¹, NRᶜ¹S(O)₂NRᶜ¹Rᵈ¹, S(O)Rᵇ¹, S(O)NRᶜ¹Rᵈ¹, S(O)₂Rᵇ¹, y S(O)₂NRᶜ¹Rᵈ¹; R¹ es C₁₋₆ alquilo; R², R³, y R⁴ se seleccionan en forma independiente entre sí entre H, halo, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, C₆₋₁₀ aril-C₁₋₄ alquilo, C₃₋₇ cicloalquil-C₁₋₄ alquilo, heteroaril-C₁₋₄ alquilo de 5 - 10 miembros, heterocicloalquil-C₁₋₄ alquilo de 4 - 10 miembros, CN, NO₂, ORᵇ², SRᵇ², C(O)Rᵇ², C(O)NRᶜ²Rᵈ², C(O)ORᵇ², OC(O)Rᵇ², OC(O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(O)Rᵇ², NRᶜ²C(O)ORᵇ², NRᶜ²C(O)NRᶜ²Rᵈ², C(=NRᵉ²)Rᵇ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²S(O)Rᵇ², NRᶜ²S(O)₂Rᵇ², NRᶜ²S(O)₂NRᶜ²Rᵈ², S(O)Rᵇ², S(O)NRᶜ²Rᵈ², S(O)₂Rᵇ², y S(O)₂NRᶜ²Rᵈ², donde dichos C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, C₆₋₁₀ aril-C₁₋₄ alquilo, C₃₋₇ cicloalquil-C₁₋₄ alquilo, heteroaril-C₁₋₄ alquilo de 5 - 10 miembros, y heterocicloalquil-C₁₋₄ alquilo de 4 - 10 miembros de R², R³, y R⁴ están opcionalmente sustituidos en cada caso con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre halo, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₁₋₆ haloalquilo, CN, NO₂, ORᵇ², SRᵇ², C(O)Rᵇ², C(O)NRᶜ²Rᵈ², C(O)ORᵇ², OC(O)Rᵇ², OC(O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(O)Rᵇ², NRᶜ²C(O)ORᵇ², NRᶜ²C(O)NRᶜ²Rᵈ², C(=NRᵉ²)Rᵇ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ2)NRᶜ²Rᵈ², NRᶜ²S(O)Rᵇ², NRᶜ²S(O)₂Rᵇ², NRᶜ²S(O)₂NRᶜ²Rᵈ², S(O)Rᵇ², S(O)NRᶜ²Rᵈ², S(O)₂Rᵇ², y S(O)₂NRᶜ²Rᵈ²; cada Rᵃ, Rᵇ, Rᶜ, Rᵈ, Rᵃ¹, Rᵇ¹, Rᶜ¹, Rᵈ¹, Rᵇ², Rᵇ², Rᶜ², y Rᵈ² se selecciona en forma independiente entre H, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, C₆₋₁₀ aril-C₁₋₄ alquilo, C₃₋₇ cicloalquil-C₁₋₄ alquilo, heteroaril-C₁₋₄ alquilo de 5 - 10 miembros, y heterocicloalquil-C₁₋₄ alquilo de 4 - 10 miembros, donde dichos C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, C₆₋₁₀ aril-C₁₋₄ alquilo, C₃₋₇ cicloalquil-C₁₋₄ alquilo, heteroaril-C₁₋₄ alquilo de 5 - 10 miembros, y heterocicloalquil-C₁₋₄ alquilo de 4 - 10 miembros de Rᵃ, Rᵇ, Rᶜ, Rᵈ, Rᵃ¹, Rᵇ¹, Rᶜ¹, Rᵈ¹, Rᵇ², Rᵇ², Rᶜ², y Rᵈ² está opcionalmente sustituido con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre halo, C₁₋₄ alquilo, C₁₋₄ haloalquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, CN, ORᵃ³, SRᵃ³, C(O)Rᵇ³, C(O)NRᶜ³Rᵈ³, C(O)ORᵃ³, OC(O)Rᵇ³, OC(O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(O)Rᵇ³, NRᶜ³C(O)NRᶜ³Rᵈ³, NRᶜ³C(O)ORᵃ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, S(O)Rᵇ³, S(O)NRᶜ³Rᵈ³, S(O)₂Rᵇ³, NRᶜ³S(O)₂Rᵇ³, NRᶜ³S(O)₂NRᶜ³Rᵈ³, y S(O)₂NRᶜ³Rᵈ³; o Rᶜ y Rᵈ junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo de 4 - 7 miembros opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre halo, C₁₋₄ alquilo, C₁₋₄ haloalquilo, CN, ORᵃ³, SRᵃ³, C(O)Rᵇ³, C(O)NRᶜ³Rᵈ³, C(O)ORᵃ³, OC(O)Rᵇ³, OC(O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(O)Rᵇ³, NRᶜ³C(O)NRᶜ³Rᵈ³, NRᶜ³C(O)ORᵃ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, S(O)Rᵇ³, S(O)NRᶜ³Rᵈ³, S(O)₂Rᵇ³, NRᶜ³S(O)₂Rᵇ³, NRᶜ³S(O)₂NRᶜ³Rᵈ³, y S(O)₂NRᶜ³Rᵈ³; o Rᶜ¹ y Rᵈ¹ junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo de 4 - 7 miembros opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre halo, C₁₋₄ alquilo, C₁₋₄ haloalquilo, CN, ORᵃ³, SRᵃ³, C(O)Rᵇ³, C(O)NRᶜ³Rᵈ³, C(O)ORᵃ³, OC(O)Rᵇ³, OC(O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(O)Rᵇ³, NRᶜ³C(O)NRᶜ³Rᵈ³, NRᶜ³C(O)ORᵃ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, S(O)Rᵇ³, S(O)NRᶜ³Rᵈ³, S(O)₂Rᵇ³, NRᶜ³S(O)₂Rᵇ³, NRᶜ³S(O)₂NRᶜ³Rᵈ³, y S(O)₂NRᶜ³Rᵈ³; o Rᶜ² y Rᵈ² junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo de 4 - 7 miembros opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre halo, C₁₋₄ alquilo, C₁₋₄ haloalquilo, CN, ORᵃ³, SRᵃ³, C(O)Rᵇ³, C(O)NRᶜ³Rᵈ³, C(O)ORᵃ³, OC(O)Rᵇ³, OC(O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(O)Rᵇ³, NRᶜ³C(O)NRᶜ³Rᵈ³, NRᶜ³C(O)ORᵃ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, S(O)Rᵇ³, S(O)NRᶜ³Rᵈ³, S(O)₂Rᵇ³, NRᶜ³S(O)₂Rᵇ³, NRᶜ³S(O)₂NRᶜ³Rᵈ³, y S(O)₂NRᶜ³Rᵈ³; cada Rᵃ³, Rᵇ³, Rᶜ³, y Rᵈ³ se selecciona en forma independiente entre H, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 6 miembros, y heterocicloalquilo de 4 - 7 miembros, donde dichos C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₆₋₁₀ arilo, C₃₋₇ cicloalquilo, heteroarilo de 5 - 6 miembros, y heterocicloalquilo de 4 - 7 miembros están opcionalmente sustituidos en cada caso con 1, 2, ó 3 sustituyentes seleccionados en forma independiente entre OH, CN, amino, halo, C₁₋₆ alquilo, C₁₋₆ alcoxi, C₁₋₆ haloalquilo, y C₁₋₆ haloalcoxi; y cada Rᵉ, Rᵉ¹, Rᵉ², y Rᵉ³ se selecciona en forma independiente entre H, C₁₋₄ alquilo, y CN; con la salvedad de que cuando X³ es CR³ y X⁴ es CR⁴, entonces el Anillo A no es un compuesto de fórmula (2). Reivindicación 31: Una composición farmacéutica caracterizada porque comprende un compuesto de cualquiera de las reivindicaciones 1 a 30, o una sal farmacéuticamente aceptable del mismo, y por lo menos un excipiente farmacéuticamente aceptable.
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| WO2021087087A1 (en) | 2019-10-30 | 2021-05-06 | Mitobridge Inc. | N-cyclohexyl-5-(thiazol-5-yl)-1h-indole-7-carboxamide derivatives and related compounds as cd38 inhibitors for increasing nad+ and for the treatment of e.g. muscular disorders |
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| IL304466A (en) | 2023-09-01 |
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| AU2022212035A1 (en) | 2023-08-03 |
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| BR112023014898A2 (pt) | 2023-10-31 |
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