AR117194A1 - Compuestos de anillos fusionados - Google Patents
Compuestos de anillos fusionadosInfo
- Publication number
- AR117194A1 AR117194A1 ARP190103302A ARP190103302A AR117194A1 AR 117194 A1 AR117194 A1 AR 117194A1 AR P190103302 A ARP190103302 A AR P190103302A AR P190103302 A ARP190103302 A AR P190103302A AR 117194 A1 AR117194 A1 AR 117194A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- alkoxy
- haloalkyl
- halo
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 14
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 8
- 125000001475 halogen functional group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 5
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 5
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 abstract 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 5
- -1 C1−6 hydroxyalkanoyl Chemical group 0.000 abstract 4
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 4
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000005466 alkylenyl group Chemical group 0.000 abstract 3
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 3
- 125000005242 carbamoyl alkyl group Chemical group 0.000 abstract 3
- 125000004995 haloalkylthio group Chemical group 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 101710113436 GTPase KRas Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 102200006538 rs121913530 Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este; caracterizado porque R¹ es un resto electrofílico capaz de formar un enlace covalente con un residuo de cisteína en la posición 12 de una proteína mutante K-Ras G12C; R² se selecciona del grupo que consiste en H, OH, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, ciclopropilo y -NHR, donde R se selecciona del grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₆, alcanoilo C₁₋₆, hidroxialcanoilo C₁₋₆, cianoalquilo C₁₋₆, alquilamino C₁₋₆, -(alquilenilo C₁₋₆)NH(CH₃)-(alquilenilo C₁₋₆)N(CH₃)₂ y -(alquilenilo C₁₋₃)(heterociclilo de 3 - 7 miembros); R³ y R⁴ se seleccionan cada uno independientemente del grupo que consiste en H, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquilamino C₁₋₆ y ciclopropilo; R⁵ se selecciona del grupo que consiste en H, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquilamino C₁₋₆ y cicloalquilo C₃₋₇, en donde al menos uno de R², R³, R⁴ y R⁵ es diferente de H; o R² y R³, R³ y R⁴, o R⁴ y R⁵, junto con los átomos a los cuales están unidos, forman un cicloalquilo C₃₋₇, heterocicloalquilo de 3 a 7 miembros, arilo C₆₋₁₄ o heteroarilo de 5 a 10 miembros; cada uno de los cuales está opcionalmente sustituido con 1 a 4 sustituyentes, en donde cada sustituyente se selecciona independientemente del grupo que consiste en OH, NH₂, halo, alquilo C₁₋₃, haloalquilo C₁₋₃, alcoxi C₁₋₃ y haloalcoxi C₁₋₃; X se selecciona del grupo que consiste en NH₂, alcoxi C₁₋₆, alquilo C₁₋₆, alquilamino C₁₋₆, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, cicloalquilo C₃₋₇, heterociclilo de 4 a 7 miembros y heterociclilamino de 4 a 7 miembros; cada uno de los cuales está opcionalmente sustituido con 1 a 4 sustituyentes, en donde cada sustituyente se selecciona independientemente del grupo que consiste en OH, NH₂, halo, ciano, carboxi, carbamoilo, alquilo C₁₋₆, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆ y heterociclilo de 4 a 7 miembros; en donde dos sustituyentes geminales se pueden tomar juntos para formar espirocicloalquilo C₃₋₇ o espiroheterociclilo de 4 a 7 miembros; Y se selecciona del grupo que consiste en -L-Y¹ o Y¹; Y¹ se selecciona del grupo que consiste en H, NH₂, halo, ciano, carbamoilo, alquenilo C₂₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con un heterociclilo de 4 a 10 miembros que se sustituye opcionalmente con 1 - 4 sustituyentes Y¹ᵃ, alquilo C₁₋₆ sustituido con un sustituyente dialquilamino C₁₋₆, alquilo C₁₋₆ sustituido con un dialquilamino ciclopropilo C₁₋₆, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, alquinilo C₂₋₆, alquilamino C₁₋₆, arilo C₆₋₁₄, arilo C₆₋₁₄ sustituido con un alquilo C₁₋₆, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇ sustituido con un dialquilamino C₁₋₆, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo de 5 a 10 miembros, heterociclilo de 4 a 10 miembros, un heterociclilo de 4 a 10 miembros sustituido con metilo, hidroxi y oxo; cada Y¹ᵃ se selecciona independientemente del grupo que consiste en halo, alquilo C₁₋₆, alcoxi C₁₋₆, heterociclilo de 3 a 7 miembros, alcoxi C₁₋₆alquilo C₁₋₆, haloalquilo C₁₋₆, oxo, hidroxi, NH₂, ciano, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, hidroxialquilo C₁₋₆ y haloalcoxi C₁₋₆; L se selecciona del grupo que consiste en un enlace, O, S y N(Lᵃ); Lᵃ se selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₃; U es C(R⁶ᵃ); V es C(R⁶ᵇ); W es C(R⁶ᶜ) o N; cada uno de R⁶ᵃ, R⁶ᵇ y R⁶ᶜ se selecciona independientemente del grupo que consiste en H, OH, NH₂, halo, ciano, carbamoilo, alquenilo C₂₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con un sustituyente heterociclilo de 4 a 10 miembros, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquinilo C₂₋₆, alquilamino C₁₋₆, arilo C₆₋₁₄, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, cicloalquilo C₃₋₇, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros; y n se selecciona del grupo que consiste en 0, 1 y 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2018114788 | 2018-11-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR117194A1 true AR117194A1 (es) | 2021-07-21 |
Family
ID=69232886
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP190103302A AR117194A1 (es) | 2018-11-09 | 2019-11-08 | Compuestos de anillos fusionados |
Country Status (22)
Country | Link |
---|---|
US (2) | US11236068B2 (es) |
EP (1) | EP3735299A2 (es) |
JP (3) | JP6941241B2 (es) |
KR (2) | KR20230147742A (es) |
CN (5) | CN118084867A (es) |
AR (1) | AR117194A1 (es) |
AU (3) | AU2019377130B2 (es) |
BR (1) | BR112021008986A2 (es) |
CA (1) | CA3087089C (es) |
CL (2) | CL2021001171A1 (es) |
CO (1) | CO2021005987A2 (es) |
CR (1) | CR20210229A (es) |
IL (2) | IL311187A (es) |
MA (1) | MA51530A (es) |
MX (1) | MX2021005428A (es) |
MY (1) | MY196726A (es) |
PE (1) | PE20211504A1 (es) |
PH (1) | PH12021551065A1 (es) |
SG (1) | SG11202103298QA (es) |
TW (2) | TWI784209B (es) |
UA (1) | UA127930C2 (es) |
WO (1) | WO2020097537A2 (es) |
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KR20220106980A (ko) | 2019-10-28 | 2022-08-01 | 머크 샤프 앤드 돔 코포레이션 | Kras g12c 돌연변이체의 소분자 억제제 |
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