PE20210154A1 - Derivados de piridincarbonilo y usos terapeuticos de los mismos como inhibidores de trpc6 - Google Patents
Derivados de piridincarbonilo y usos terapeuticos de los mismos como inhibidores de trpc6Info
- Publication number
- PE20210154A1 PE20210154A1 PE2020000424A PE2020000424A PE20210154A1 PE 20210154 A1 PE20210154 A1 PE 20210154A1 PE 2020000424 A PE2020000424 A PE 2020000424A PE 2020000424 A PE2020000424 A PE 2020000424A PE 20210154 A1 PE20210154 A1 PE 20210154A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- pyridin
- methoxy
- trpc6
- Prior art date
Links
- -1 PYRIDINCARBONYL Chemical class 0.000 title abstract 2
- 102000003623 TRPC6 Human genes 0.000 title 1
- 108050001421 Transient receptor potential channel, canonical 6 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000001225 therapeutic effect Effects 0.000 title 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- QDKWLJJOYIFEBS-UHFFFAOYSA-N 1-fluoro-4-$l^{1}-oxidanylbenzene Chemical group [O]C1=CC=C(F)C=C1 QDKWLJJOYIFEBS-UHFFFAOYSA-N 0.000 abstract 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract 1
- 239000005977 Ethylene Substances 0.000 abstract 1
- 102000004310 Ion Channels Human genes 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 206010063837 Reperfusion injury Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000000747 cardiac effect Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 208000012947 ischemia reperfusion injury Diseases 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 208000019423 liver disease Diseases 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 201000006938 muscular dystrophy Diseases 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000000241 respiratory effect Effects 0.000 abstract 1
- 230000001052 transient effect Effects 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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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
-
- 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
- A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- 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
- C07D487/08—Bridged 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
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Se refiere a composiciones, compuestos farmaceuticos y a metodos para el tratamiento de estados cardiacos y respiratorios, enfermedad renal, enfermedad hepatica, distrofia muscular, trastornos fibroticos, dolor, isquemia o lesion por isquemia-reperfusion, y cancer, asi como para inhibir el canal ionico C6 receptor de potencial transitorio (TRPC6). Esta referido a compuestos de Formula I, en donde: L esta ausente o es metileno o etileno; Y es CH o N; A es CH o N; R1 es alquilo, fenilo, cicloalquilo; R2 es H, alquilo C1-6, OCF3, cicloalquilo, alquilo O, cicloalquilo O; R3 es H, alquilo C1-6, cicloalquilo C3-6, cicloalquilo OC3-6; R4 y R5 son H o alquilo C1-6; R6 es H, alquilo C1-6, CN, CF3, OCF3, cicloalquilo C3-6, alquilo OC1-6, y cicloalquilo OC3-6; R7 es H o alquilo OC1-6. Entre los compuestos preferidos tenemos: [4-(6-Amino-4-metoxi-piridin-3- il)-piperazin-1-il]-[5-(4-fluoro-fenoxi)-4-metoxi-piridin-2-il]- metanona; (6-Amino-3',4',5',6'-tetrahidro- 2'H-[3,4']bipiridinil-1''-il)-(4- metoxi-5-fenoxi-piridin-2-il)- metanona; entre otros.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762577883P | 2017-10-27 | 2017-10-27 | |
| US201862628313P | 2018-02-09 | 2018-02-09 | |
| PCT/EP2018/079276 WO2019081637A1 (en) | 2017-10-27 | 2018-10-25 | CARBONYL PYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USES AS TRPC6 INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20210154A1 true PE20210154A1 (es) | 2021-01-26 |
Family
ID=64270818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020000424A PE20210154A1 (es) | 2017-10-27 | 2018-10-25 | Derivados de piridincarbonilo y usos terapeuticos de los mismos como inhibidores de trpc6 |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US10889568B2 (es) |
| EP (2) | EP3786160B1 (es) |
| JP (2) | JP7217273B6 (es) |
| KR (2) | KR20200125758A (es) |
| CN (1) | CN111527078B (es) |
| AU (2) | AU2018355743B2 (es) |
| CA (1) | CA3078769A1 (es) |
| CL (2) | CL2020001097A1 (es) |
| CY (1) | CY1126109T1 (es) |
| DK (2) | DK3700902T3 (es) |
| ES (2) | ES2946274T3 (es) |
| FI (1) | FI3700902T3 (es) |
| HR (2) | HRP20230502T1 (es) |
| HU (2) | HUE062460T2 (es) |
| IL (2) | IL274039B (es) |
| LT (2) | LT3700902T (es) |
| MX (1) | MX387232B (es) |
| MY (1) | MY202126A (es) |
| NZ (1) | NZ763816A (es) |
| PE (1) | PE20210154A1 (es) |
| PH (1) | PH12020550503A1 (es) |
| PL (2) | PL3786160T3 (es) |
| PT (2) | PT3700902T (es) |
| RS (2) | RS64271B1 (es) |
| SA (1) | SA520411843B1 (es) |
| SG (2) | SG10202011632RA (es) |
| SI (2) | SI3786160T1 (es) |
| TW (2) | TWI780246B (es) |
| UA (1) | UA128474C2 (es) |
| WO (1) | WO2019081637A1 (es) |
| ZA (1) | ZA202002372B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS64271B1 (sr) * | 2017-10-27 | 2023-07-31 | Boehringer Ingelheim Int | Inhibitori trpc6 |
| CN111770918B (zh) * | 2018-02-15 | 2024-02-27 | 勃林格殷格翰国际公司 | Trpc6的抑制剂 |
| EP3752503A1 (en) * | 2018-02-16 | 2020-12-23 | Boehringer Ingelheim International GmbH | Inhibitors of trpc6 |
| IL315313A (en) * | 2018-08-24 | 2024-10-01 | Xeniopro GmbH | Aromatic molecules for use in the treatment of pathological conditions |
| WO2020208002A1 (en) * | 2019-04-12 | 2020-10-15 | Boehringer Ingelheim International Gmbh | Inhibitors of trpc6 |
| JP7594274B2 (ja) | 2019-10-24 | 2024-12-04 | 国立大学法人大阪大学 | 難聴の予防および／または治療用医薬組成物 |
| WO2021160625A1 (en) | 2020-02-11 | 2021-08-19 | Klinikum Rechts Der Isar | Administration of calcium channel trpc6 inhibitors using balloons, stents or other medical devices |
| CN115379841A (zh) * | 2020-04-16 | 2022-11-22 | 勃林格殷格翰国际有限公司 | 治疗呼吸系统病症的trpc6抑制剂 |
| AR121846A1 (es) | 2020-04-16 | 2022-07-13 | Teijin Pharma Ltd | Derivado de arilo o heteroarilo |
| CN113105318B (zh) * | 2021-02-23 | 2022-05-20 | 中山大学 | 一种2,2-二氟环丁烷-1-羧酸的制备方法及应用 |
| CN119751348A (zh) | 2021-10-15 | 2025-04-04 | 勃林格殷格翰国际有限公司 | 用于治疗脓毒症的trpc6抑制性化合物 |
| JP2025023360A (ja) * | 2021-12-06 | 2025-02-17 | 国立大学法人 熊本大学 | Ｔｒｐｃ６の発現を抑制する方法 |
| WO2025042707A1 (en) | 2023-08-18 | 2025-02-27 | Boehringer Ingelheim International Gmbh | Inhibitors of trpc6 for treating focal segmental glomerulosclerosis |
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