PE20231986A1 - Compuesto de heteroarilcarboxamida - Google Patents
Compuesto de heteroarilcarboxamidaInfo
- Publication number
- PE20231986A1 PE20231986A1 PE2023001705A PE2023001705A PE20231986A1 PE 20231986 A1 PE20231986 A1 PE 20231986A1 PE 2023001705 A PE2023001705 A PE 2023001705A PE 2023001705 A PE2023001705 A PE 2023001705A PE 20231986 A1 PE20231986 A1 PE 20231986A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- fluorophenoxy
- carboxamide
- pyrazole
- trifluoromethyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- -1 -O-(alkyl) Chemical group 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 230000004913 activation Effects 0.000 abstract 1
- 238000009175 antibody therapy Methods 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 210000002865 immune cell Anatomy 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 abstract 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
Classifications
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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
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed 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
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
-
- 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
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (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)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Esta referido a derivados de heteroarilcarboxamida de Formula I, en donde: R2 es cicloalquilo, -O-(alquilo), halogeno-alquilo, halogeno o fenilo; R3 es fenilo, cicloalquilo, piridilo o un anillo heterociclico, cualquiera de ellos opcionalmente sustituido; R4 es H, F; L1 es un enlace, O, NH; y, A y B son como se indica a continuacion. Entre los compuestos preferidos tenemos los siguientes: N-{2-[(3S)-3-(aminometil)piperidin-1-il]-4-(2-fluorofenoxi)-3-(trifluorometil)fenil}- 1-(2,2-difluoroetil)-1H-pirazol-3-carboxamida; N-[4-(2-fluorofenoxi)-2-{(3S)-4-metil-3-[(metilamino)metil]piperazin1-il}-3- (trifluorometil)fenil]-1-(piridazin-4-il)-1H-pirazol-3-carboxamida; entre otros. Estos compuestos tienen un efecto inhibidor Xi de DGK y se emplean en el tratamiento del cancer relacionado con la activacion de celulas inmunitarias o cancer resistente a la terapia con anticuerpo anti-PD-1/anticuerpo anti-PD-L1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020197899 | 2020-11-30 | ||
| PCT/JP2021/043540 WO2022114164A1 (ja) | 2020-11-30 | 2021-11-29 | ヘテロアリールカルボキシアミド化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20231986A1 true PE20231986A1 (es) | 2023-12-12 |
Family
ID=81754515
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001705A PE20231986A1 (es) | 2020-11-30 | 2021-11-29 | Compuesto de heteroarilcarboxamida |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US20240043403A1 (es) |
| EP (1) | EP4253373A1 (es) |
| JP (1) | JP7397452B2 (es) |
| KR (1) | KR20230116838A (es) |
| CN (1) | CN116528864A (es) |
| AR (1) | AR124172A1 (es) |
| AU (1) | AU2021389180A1 (es) |
| CA (1) | CA3203285A1 (es) |
| CL (1) | CL2023001534A1 (es) |
| CO (1) | CO2023008271A2 (es) |
| CR (1) | CR20230415A (es) |
| DO (1) | DOP2023000107A (es) |
| EC (1) | ECSP23048974A (es) |
| IL (1) | IL303209A (es) |
| MX (1) | MX2023006318A (es) |
| PE (1) | PE20231986A1 (es) |
| TW (1) | TW202229256A (es) |
| WO (1) | WO2022114164A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR120896A1 (es) * | 2019-12-25 | 2022-03-30 | Astellas Pharma Inc | COMPUESTO DE PIRIDAZINIL-TIAZOLCARBOXAMIDA COMO INHIBIDORES DE DGKz |
| WO2023248109A1 (en) | 2022-06-20 | 2023-12-28 | Astellas Pharma Inc. | Methods for treating patients with locally advanced and/or metastatic solid tumors using a dgk zeta inhibitor |
| WO2024108100A1 (en) * | 2022-11-18 | 2024-05-23 | Incyte Corporation | Heteroaryl fluoroalkenes as dgk inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7381401B2 (en) | 2004-01-08 | 2008-06-03 | The University Of Chicago | T cell anergy is reversed by active Ras and regulated by diacylglycerol kinase |
| NZ556732A (en) | 2005-01-25 | 2011-11-25 | Synta Pharmaceuticals Corp | Pyrazine compounds for inflammation and immune-related uses |
| EP1983980A4 (en) * | 2006-01-25 | 2010-05-05 | Synta Pharmaceuticals Corp | THIAZOL AND THIADIAZOL COMPOUNDS FOR USES IN RELATION TO INFLAMMATION AND IMMUNITY |
| MX2008013400A (es) | 2006-04-19 | 2008-11-10 | Astellas Pharma Inc | Derivado de azolcarboxamida. |
| EP2078003B1 (en) | 2006-10-31 | 2017-03-08 | Merck Sharp & Dohme Corp. | Anilinopiperazine derivatives and methods of use thereof |
| WO2019046944A1 (en) * | 2017-09-06 | 2019-03-14 | Propellon Therapeutics Inc. | INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN |
| RS64641B1 (sr) | 2018-06-27 | 2023-10-31 | Bristol Myers Squibb Co | Supstituisana jedinjenja naftiridinona korisna kao aktivatori t ćelija |
| AR120896A1 (es) | 2019-12-25 | 2022-03-30 | Astellas Pharma Inc | COMPUESTO DE PIRIDAZINIL-TIAZOLCARBOXAMIDA COMO INHIBIDORES DE DGKz |
-
2021
- 2021-11-29 JP JP2022565480A patent/JP7397452B2/ja active Active
- 2021-11-29 EP EP21898136.3A patent/EP4253373A1/en active Pending
- 2021-11-29 AR ARP210103290A patent/AR124172A1/es unknown
- 2021-11-29 CR CR20230415A patent/CR20230415A/es unknown
- 2021-11-29 TW TW110144382A patent/TW202229256A/zh unknown
- 2021-11-29 PE PE2023001705A patent/PE20231986A1/es unknown
- 2021-11-29 KR KR1020237021502A patent/KR20230116838A/ko unknown
- 2021-11-29 CA CA3203285A patent/CA3203285A1/en active Pending
- 2021-11-29 MX MX2023006318A patent/MX2023006318A/es unknown
- 2021-11-29 WO PCT/JP2021/043540 patent/WO2022114164A1/ja active Application Filing
- 2021-11-29 AU AU2021389180A patent/AU2021389180A1/en active Pending
- 2021-11-29 IL IL303209A patent/IL303209A/en unknown
- 2021-11-29 CN CN202180080083.8A patent/CN116528864A/zh active Pending
- 2021-11-29 US US18/254,829 patent/US20240043403A1/en active Pending
-
2023
- 2023-05-29 CL CL2023001534A patent/CL2023001534A1/es unknown
- 2023-05-29 DO DO2023000107A patent/DOP2023000107A/es unknown
- 2023-06-23 CO CONC2023/0008271A patent/CO2023008271A2/es unknown
- 2023-06-29 EC ECSENADI202348974A patent/ECSP23048974A/es unknown
- 2023-11-28 US US18/521,400 patent/US20240101532A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20230116838A (ko) | 2023-08-04 |
| CO2023008271A2 (es) | 2023-07-21 |
| ECSP23048974A (es) | 2023-07-31 |
| TW202229256A (zh) | 2022-08-01 |
| AR124172A1 (es) | 2023-02-22 |
| AU2021389180A9 (en) | 2024-06-13 |
| JPWO2022114164A1 (es) | 2022-06-02 |
| DOP2023000107A (es) | 2023-07-16 |
| CA3203285A1 (en) | 2022-06-02 |
| EP4253373A1 (en) | 2023-10-04 |
| CL2023001534A1 (es) | 2023-11-10 |
| JP7397452B2 (ja) | 2023-12-13 |
| AU2021389180A1 (en) | 2023-06-29 |
| CR20230415A (es) | 2023-09-08 |
| MX2023006318A (es) | 2023-06-14 |
| WO2022114164A1 (ja) | 2022-06-02 |
| US20240043403A1 (en) | 2024-02-08 |
| US20240101532A1 (en) | 2024-03-28 |
| CN116528864A (zh) | 2023-08-01 |
| IL303209A (en) | 2023-07-01 |
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