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
- -1 KETONE COMPOUNDS Chemical class 0.000 title abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 5
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 229910052736 halogen 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
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000004001 thioalkyl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Chemical group 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 102100021009 Cytochrome b-c1 complex subunit Rieske, mitochondrial Human genes 0.000 abstract 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- 101000643956 Homo sapiens Cytochrome b-c1 complex subunit Rieske, mitochondrial Proteins 0.000 abstract 1
- 101001099199 Homo sapiens RalA-binding protein 1 Proteins 0.000 abstract 1
- 101001109145 Homo sapiens Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 229910052805 deuterium Inorganic materials 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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]
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 (29)
| Country | Link |
|---|---|
| US (2) | US11098058B2 (es) |
| EP (2) | EP4397309A2 (es) |
| JP (2) | JP7258843B2 (es) |
| KR (2) | KR20240065201A (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) |
| ES (1) | ES2973661T3 (es) |
| FI (1) | FI3652178T3 (es) |
| HR (1) | HRP20240354T1 (es) |
| HU (1) | HUE065793T2 (es) |
| IL (2) | IL271981B (es) |
| LT (1) | LT3652178T (es) |
| MA (1) | MA49560B1 (es) |
| PH (1) | PH12020500105A1 (es) |
| PL (1) | PL3652178T3 (es) |
| PT (1) | PT3652178T (es) |
| RS (1) | RS65308B1 (es) |
| SG (1) | SG11202000333UA (es) |
| SI (1) | SI3652178T1 (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 |
|---|---|---|---|---|
| US11071721B2 (en) * | 2016-12-02 | 2021-07-27 | Genentech, Inc. | Bicyclic amide compounds and methods of use thereof |
| EP4397309A2 (en) | 2017-07-14 | 2024-07-10 | F. Hoffmann-La Roche AG | Bicyclic ketone compounds and methods of use thereof |
| RU2020115915A (ru) | 2017-10-31 | 2021-12-01 | Ф. Хоффманн-Ля Рош Аг | Бициклические сульфоны и сульфоксиды и способы их применения |
| WO2021198981A1 (en) | 2020-04-01 | 2021-10-07 | Janssen Biopharma, Inc. | Antiviral compounds and uses thereof |
| CN115715285A (zh) * | 2020-04-27 | 2023-02-24 | 奧土择破利悟 | 作为ubr盒结构域配体的化合物 |
| CA3214802A1 (en) | 2021-04-02 | 2022-10-06 | Genentech, Inc. | Processes for making bicyclic ketone compounds |
| 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 |
| US20240025912A1 (en) * | 2022-05-19 | 2024-01-25 | Merck Sharp & Dohme Llc | Ripk1 inhibitors and methods of use |
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| RU2014148732A (ru) | 2012-05-22 | 2016-07-20 | Ф. Хоффманн-Ля Рош Аг | Замещенные дипиридиламины и их применение |
| RU2015131314A (ru) | 2013-01-18 | 2017-02-27 | Ф. Хоффманн-Ля Рош Аг | 3-замещенные пиразолы и их применение в качестве ингибиторов dlk |
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| RU2015147601A (ru) | 2013-05-01 | 2017-06-05 | Ф. Хоффманн-Ля Рош Аг | С-связанные гетероциклоалкилзамещенные пиримидины и их применения |
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| US11071721B2 (en) | 2016-12-02 | 2021-07-27 | Genentech, Inc. | Bicyclic amide compounds and methods of use thereof |
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| CN110169087B (zh) | 2017-01-05 | 2021-04-20 | 微软技术许可有限责任公司 | 重定向音频输出 |
| EP4397309A2 (en) | 2017-07-14 | 2024-07-10 | F. Hoffmann-La Roche AG | Bicyclic ketone compounds and methods of use thereof |
| SG11202003283TA (en) | 2017-10-11 | 2020-05-28 | Hoffmann La Roche | Bicyclic compounds for use as rip1 kinase inhibitors |
| RU2020115915A (ru) | 2017-10-31 | 2021-12-01 | Ф. Хоффманн-Ля Рош Аг | Бициклические сульфоны и сульфоксиды и способы их применения |
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