AR112274A1 - Compuestos bicíclicos de cetona y sus métodos de uso - Google Patents
Compuestos bicíclicos de cetona y sus métodos de usoInfo
- Publication number
- AR112274A1 AR112274A1 ARP180101941A AR112274A1 AR 112274 A1 AR112274 A1 AR 112274A1 AR P180101941 A ARP180101941 A AR P180101941A AR 112274 A1 AR112274 A1 AR 112274A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- ring
- alkoxy
- membered
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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]
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/12—Radicals substituted by oxygen atoms
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- 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
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
Abstract
Composiciones farmacéuticas que incluyen los compuestos y su uso en el tratamiento de enfermedades mediadas por RIP1. Reivindicación 1: Un compuesto de fórmula (1), o sus sales farmacéuticamente aceptables, caracterizado porque: R¹ se selecciona entre el grupo que consiste en alquilo C₁₋₆ cicloalquilo C₃₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, alquilo C₁₋₆-N(RN)₂, fenilo, bencilo, heterociclilo de 4 a 8 miembros y heteroarilo de 5 a 6 miembros; en donde R¹ está unido a un carbonilo adyacente por un átomo de carbono, y en donde R¹ está opcionalmente sustituido con uno o dos sustituyentes seleccionados entre el grupo que consiste en F, Cl, Br, alquilo C₁₋₆, cicloalquilo C₃₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, alquilo C₁₋₆-N(RN)₂, hidroxilo, hidroximetilo, ciano, cianometilo, cianoetilo, alquilo C(O)C₁₋₆ fenilo, bencilo, CH₂-(cicloalquilo C₃₋₆), heteroarilo de 5 a 6 miembros, y CH₂-(heteroarilo de 5 a 6 miembros); cada RN se selecciona en forma independiente entre el grupo que consiste en H, alquilo C₁₋₆, cicloalquilo C₃₋₆, alcoxi C₁₋₆, y haloalquilo C₁₋₆; o dos RN, junto con el N adyacente, pueden formar un anillo de 4 a 6 miembros; un anillo A es un heteroarilo de 5 miembros que tiene los únicos heteroátomos, ya sea (i) dos o tres átomos de nitrógeno, (ii) un átomo de nitrógeno y un átomo de oxígeno, o (iii) un átomo de nitrógeno y un átomo de azufre; en donde el anillo A está unido al carbonilo adyacente por un átomo de carbono; y el anillo B es un cicloalquilo de 4 a 8 miembros, o un heterociclilo de 4 a 8 miembros que tiene entre 1 y 3 heteroátomos seleccionados entre el grupo que consiste en nitrógeno, oxígeno y azufre; en donde el anillo B está sustituido de acuerdo con (a), (b) o ambos, (a) y (b): (a) de 1 a 2 sustituyentes seleccionados entre el grupo que consiste en halógeno, deuterio, hidroxi, alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, tioalquilo C₁₋₆, alquilo C₁₋₆-N(RN)₂, y ciano; en donde, dos sustituyentes de alquilo C₁₋₆ pueden formar, juntos, un anillo espirocíclico o en puente; y en donde si se sustituye un átomo de nitrógeno en el anillo B, el sustituyente no es halógeno, ciano, ni un alcoxi C₁₋₆, haloalcoxi C₁₋₆ ni tioalquilo C₁₋₆ con un átomo de oxígeno o de azufre directamente unido al átomo de nitrógeno; (b) sustituyente seleccionado entre el grupo que consisten en alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, tioalquilo C₁₋₆, alquilo C₁₋₆-N(RN)₂, fenilo, bencilo, CH₂-(cicloalquilo C₃₋₆), CH₂CH₂-(cicloalquilo C₃₋₆), CH₂-(heterociclilo de 4 a 6 miembros), CH₂CH₂-(heterociclilo de 4 a 6 miembros), heteroarilo de 5 a 6 miembros, y CH₂-(heteroarilo de 5 a 6 miembros); en donde, cuando está presente un anillo de fenilo o un anillo de heteroarilo de 5 a 6 miembros, este puede sustituirse por 1 a 3 sustituyentes seleccionados entre el grupo que consiste en halógeno, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, haloalcoxi C₁₋₄, ciano, y ciclopropilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762532767P | 2017-07-14 | 2017-07-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR112274A1 true AR112274A1 (es) | 2019-10-09 |
Family
ID=62916677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101941 AR112274A1 (es) | 2017-07-14 | 2018-07-12 | Compuestos bicíclicos de cetona y sus métodos de uso |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US11098058B2 (es) |
| EP (1) | EP3652178B1 (es) |
| JP (2) | JP7258843B2 (es) |
| KR (1) | KR20200030558A (es) |
| CN (1) | CN110914271A (es) |
| AR (1) | AR112274A1 (es) |
| AU (3) | AU2018300043B2 (es) |
| BR (1) | BR112020000771A2 (es) |
| CA (2) | CA3185865A1 (es) |
| CL (1) | CL2020000101A1 (es) |
| CO (1) | CO2020000134A2 (es) |
| CR (1) | CR20200002A (es) |
| DK (1) | DK3652178T3 (es) |
| FI (1) | FI3652178T3 (es) |
| IL (2) | IL271981B (es) |
| LT (1) | LT3652178T (es) |
| MA (1) | MA49560A (es) |
| PH (1) | PH12020500105A1 (es) |
| PT (1) | PT3652178T (es) |
| SG (1) | SG11202000333UA (es) |
| TW (1) | TWI805595B (es) |
| UA (1) | UA125448C2 (es) |
| WO (1) | WO2019012063A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR110282A1 (es) * | 2016-12-02 | 2019-03-13 | Hoffmann La Roche | Compuestos de amida bicíclica y uso de éstos en el tratamiento de enfermedades mediadas por rip1 |
| MA49560A (fr) | 2017-07-14 | 2020-05-20 | Hoffmann La Roche | Composés cétoniques bicycliques et leurs procédés d'utilisation |
| SG11202002877RA (en) | 2017-10-31 | 2020-04-29 | Hoffmann La Roche | Bicyclic sulfones and sulfoxides and methods of use thereof |
| WO2021198981A1 (en) | 2020-04-01 | 2021-10-07 | Janssen Biopharma, Inc. | Antiviral compounds and uses thereof |
| EP4144720A1 (en) * | 2020-04-27 | 2023-03-08 | Autotac Inc. | Compound as ubr-box domain ligand |
| BR112023020229A2 (pt) | 2021-04-02 | 2023-11-14 | Hoffmann La Roche | Processos para a preparação de um composto bicíclico de cetona quiral, composto de n-amino lactama quiral, composto de sal imidato e composto hidroxicetoéster, composto, ou um sal farmaceuticamente aceitável do mesmo e invenção |
| WO2023039795A1 (zh) * | 2021-09-16 | 2023-03-23 | 维泰瑞隆（北京）生物科技有限公司 | Rip1激酶抑制剂及其用途 |
| WO2023225041A1 (en) * | 2022-05-19 | 2023-11-23 | Merck Sharp & Dohme Llc | Ripk1 inhibitors and methods of use |
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| CN108602809B (zh) | 2015-12-04 | 2022-09-30 | 戴纳立制药公司 | 异噁唑烷衍生的受体相互作用蛋白激酶1(ripk 1)的抑制剂 |
| US10961258B2 (en) | 2015-12-21 | 2021-03-30 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
| CR20180413A (es) | 2016-02-05 | 2018-12-04 | Denali Therapeutics Inc | Inhibidores de la proteína quinasa 1 que interactua con el receptor |
| AR110282A1 (es) | 2016-12-02 | 2019-03-13 | Hoffmann La Roche | Compuestos de amida bicíclica y uso de éstos en el tratamiento de enfermedades mediadas por rip1 |
| US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
| WO2018128908A1 (en) | 2017-01-05 | 2018-07-12 | Microsoft Technology Licensing, Llc | Redirecting audio output |
| MA49560A (fr) | 2017-07-14 | 2020-05-20 | Hoffmann La Roche | Composés cétoniques bicycliques et leurs procédés d'utilisation |
| RU2020114670A (ru) | 2017-10-11 | 2021-11-12 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения для применения в качестве ингибиторов rip1 киназы |
| SG11202002877RA (en) | 2017-10-31 | 2020-04-29 | Hoffmann La Roche | Bicyclic sulfones and sulfoxides and methods of use thereof |
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