PE20220346A1 - Derivados de 1,3-fenil heteroarilo sustituidos y su uso en el tratamiento de enfermedades - Google Patents
Derivados de 1,3-fenil heteroarilo sustituidos y su uso en el tratamiento de enfermedadesInfo
- Publication number
- PE20220346A1 PE20220346A1 PE2022000246A PE2022000246A PE20220346A1 PE 20220346 A1 PE20220346 A1 PE 20220346A1 PE 2022000246 A PE2022000246 A PE 2022000246A PE 2022000246 A PE2022000246 A PE 2022000246A PE 20220346 A1 PE20220346 A1 PE 20220346A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- phenyl
- optionally substituted
- ring
- halogen
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 201000010099 disease Diseases 0.000 title abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 23
- 229910052736 halogen Chemical group 0.000 abstract 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical compound C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 abstract 4
- FTNJQNQLEGKTGD-UHFFFAOYSA-N 1,3-benzodioxole Chemical compound C1=CC=C2OCOC2=C1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 abstract 2
- 208000025678 Ciliary Motility disease Diseases 0.000 abstract 2
- 201000003883 Cystic fibrosis Diseases 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005037 alkyl phenyl group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 201000009266 primary ciliary dyskinesia Diseases 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- -1 2-(3-(5-((dicyclopropylmethyl)carbamoyl)-1-(3,3,3-trifluoro-2-hydroxypropyl)- 1H-pyrazol-3-yl)phenyl)oxazole-5 -carbonyl Chemical group 0.000 abstract 1
- 206010006458 Bronchitis chronic Diseases 0.000 abstract 1
- VOKNONSNZDAQFF-UHFFFAOYSA-N C1(CCCC1)NC(=O)C1=CN=C(O1)C1=CC(=CC=C1)C1=NN(C(=C1)C(NC1CCCC1)=O)CCCO Chemical compound C1(CCCC1)NC(=O)C1=CN=C(O1)C1=CC(=CC=C1)C1=NN(C(=C1)C(NC1CCCC1)=O)CCCO VOKNONSNZDAQFF-UHFFFAOYSA-N 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 206010057190 Respiratory tract infections Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 230000001580 bacterial effect Effects 0.000 abstract 1
- 201000009267 bronchiectasis Diseases 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 208000007451 chronic bronchitis Diseases 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 201000005296 lung carcinoma Diseases 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 150000002825 nitriles Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 208000020029 respiratory tract infectious disease Diseases 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 230000003612 virological effect Effects 0.000 abstract 1
Classifications
-
- 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
- C07D413/10—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 linked by a carbon chain containing aromatic 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
- A61K31/41—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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles 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
- A61K31/435—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
- A61K31/535—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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invencion se refiere a compuestos heterociclicos de la formula (I), donde el anillo A es un anillo heteroarilo de 5 miembros que contiene 2 heteroatomos seleccionados de N y O; el anillo B es un anillo heteroarilo de 5 miembros que contiene 2 o 3 heteroatomos seleccionados de N, S y O, o es un heteroarilo de 6 miembros que contiene 1 o 2 heteroatomos seleccionados de N; R1 es hidrogeno o halogeno; R2 es -CO-NH-CR2aR2b-CO-O-R2c, -CO-NH-CR2fR2eR2g, entre otros; R2a es H, (C1-C4)alquilo, fenilo, entre otros; R2b es H, (C1-C4)alquilo, entre otros; R2e es H, (C1-C4)alquilo o anillo (C3-C6)cicloalquilo; R2f es H, (C1-C4)alquilo o anillo (C3-C6)cicloalquilo opcionalmente sustituido con (C1-C4)alquilo, entre otros; R2g es H, (C1-C4)alquilo, un resto fusionado seleccionado de benzo[d][1,3]dioxol e indolin-2-ona, donde dicho resto fusionado esta opcionalmente sustituido con halogeno o (C1-C4)alquilo, (C3-C6)heterocicloalquilo que contiene 1 o 2 heteroatomos seleccionados de N y O, -(C0-C2)alquilo-fenilo en donde dicho fenilo esta opcionalmente sustituido con halogeno o (C1-C4)alquilo; R2c es (C1-C4)alquilo, (C2-C4)alquenilo o bencilo; R3 es H, (C1-C5)alquilo o un heterociclo saturado de 4 a 6 miembros que contiene O; en donde dicho (C1-C5)alquilo esta opcionalmente sustituido con hidroxilo, (C1-C5)alcoxi, halogeno, entre otros; R4 es -CO-NH-CR4aR4b-CO-O-R4c, -CO-NH-CR4fR4eR4g, entre otros; R4a es H, (C1-C4)alquilo o fenilo, en donde dicho (C1-C4)alquilo esta opcionalmente sustituido con halogeno, (C3-C6)cicloalquilo, fenilo, -O-(C1-C4)alquilo o -S- (C1-C4)alquilo; y R4b es H o (C1-C4)alquilo, entre otros; R4c es (C1-C4)alquilo, (C2-C4)alquenilo o bencilo; R4e es H, (C1-C4)alquilo, (C1-C4)alcoxi o anillo (C3-C6)cicloalquilo; R4f es H, (C1-C4)alquilo o anillo (C3-C6)cicloalquilo opcionalmente sustituido con nitrilo o (C1-C4)alquilo, entre otros; R4g es H, (C1-C4)alquilo, un resto fusionado seleccionado de benzo[d][1,3]dioxol e indolin-2-ona, donde dicho resto fusionado esta opcionalmente sustituido con halogeno o (C1-C4)alquilo, (C3-C6)heterocicloalquilo que contiene 1 o 2 heteroatomos seleccionados de N y O, -(C0-C2)alquilo-fenilo en donde dicho fenilo esta opcionalmente sustituido con halogenos; R5 es H o (C1-C4)alquilo, en donde dicho (C1-C4)alquilo esta opcionalmente sustituido con (C3-C6)cicloalquilo, fenilo, -O-(C1-C4)alquilo o -S-(C1-C4)alquilo. Son compuestos especificos: metil (2-(3-(5-((diciclopropilmetil)carbamoil)-1-(3,3,3-trifluoro-2-hidroxipropil)- 1H-pirazol-3-il)fenilo)oxazol-5-carbonil)-L-valinato; N-ciclopentil-2-(3-(5-(ciclopentilcarbamoil)-1-(3-hidroxipropil)-1H-pirazol-3- il)fenilo)oxazol-5-carboxamida; entre otros. Dichos compuestos modulan la actividad de TMEM16a y son utiles en el tratamiento de enfermedades o trastornos que incluyen EPOC, bronquiectasia, asma, fibrosis quistica, disquinesia ciliar primaria, bronquitis cronica, fibrosis quistica, disquinesia ciliar primaria, infecciones del tracto respiratorio (aguda y cronica; viral y bacteriana), carcinoma de pulmon.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962892664P | 2019-08-28 | 2019-08-28 | |
| PCT/IB2020/057905 WO2021038426A1 (en) | 2019-08-28 | 2020-08-24 | Substituted 1,3-phenyl heteroaryl derivatives and their use in the treatment of disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220346A1 true PE20220346A1 (es) | 2022-03-14 |
Family
ID=72292591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022000246A PE20220346A1 (es) | 2019-08-28 | 2020-08-24 | Derivados de 1,3-fenil heteroarilo sustituidos y su uso en el tratamiento de enfermedades |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20220306617A1 (es) |
| EP (1) | EP4021572A1 (es) |
| JP (1) | JP2022547427A (es) |
| KR (1) | KR20220052934A (es) |
| CN (1) | CN114341132A (es) |
| AR (1) | AR119819A1 (es) |
| AU (1) | AU2020338971B2 (es) |
| BR (1) | BR112022002569A2 (es) |
| CA (1) | CA3146109A1 (es) |
| CO (1) | CO2022001387A2 (es) |
| CR (1) | CR20220060A (es) |
| DO (1) | DOP2022000034A (es) |
| EC (1) | ECSP22011156A (es) |
| IL (1) | IL289616A (es) |
| JO (1) | JOP20220044A1 (es) |
| MX (1) | MX2022002374A (es) |
| PE (1) | PE20220346A1 (es) |
| TW (1) | TWI753550B (es) |
| UY (1) | UY38860A (es) |
| WO (1) | WO2021038426A1 (es) |
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-
2020
- 2020-08-24 EP EP20764788.4A patent/EP4021572A1/en active Pending
- 2020-08-24 PE PE2022000246A patent/PE20220346A1/es unknown
- 2020-08-24 JP JP2022513293A patent/JP2022547427A/ja active Pending
- 2020-08-24 CN CN202080059610.2A patent/CN114341132A/zh active Pending
- 2020-08-24 AU AU2020338971A patent/AU2020338971B2/en not_active Expired - Fee Related
- 2020-08-24 AR ARP200102380A patent/AR119819A1/es unknown
- 2020-08-24 BR BR112022002569A patent/BR112022002569A2/pt unknown
- 2020-08-24 KR KR1020227006043A patent/KR20220052934A/ko unknown
- 2020-08-24 MX MX2022002374A patent/MX2022002374A/es unknown
- 2020-08-24 US US17/638,106 patent/US20220306617A1/en active Pending
- 2020-08-24 JO JOP/2022/0044A patent/JOP20220044A1/ar unknown
- 2020-08-24 CA CA3146109A patent/CA3146109A1/en active Pending
- 2020-08-24 CR CR20220060A patent/CR20220060A/es unknown
- 2020-08-24 UY UY0001038860A patent/UY38860A/es unknown
- 2020-08-24 WO PCT/IB2020/057905 patent/WO2021038426A1/en active Application Filing
- 2020-08-26 TW TW109129135A patent/TWI753550B/zh active
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2022
- 2022-01-04 IL IL289616A patent/IL289616A/en unknown
- 2022-02-10 DO DO2022000034A patent/DOP2022000034A/es unknown
- 2022-02-11 EC ECSENADI202211156A patent/ECSP22011156A/es unknown
- 2022-02-11 CO CONC2022/0001387A patent/CO2022001387A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022547427A (ja) | 2022-11-14 |
| IL289616A (en) | 2022-03-01 |
| JOP20220044A1 (ar) | 2023-01-30 |
| AR119819A1 (es) | 2022-01-12 |
| TWI753550B (zh) | 2022-01-21 |
| US20220306617A1 (en) | 2022-09-29 |
| CO2022001387A2 (es) | 2022-03-18 |
| CA3146109A1 (en) | 2021-03-04 |
| TW202122386A (zh) | 2021-06-16 |
| DOP2022000034A (es) | 2022-03-15 |
| BR112022002569A2 (pt) | 2022-07-19 |
| CN114341132A (zh) | 2022-04-12 |
| AU2020338971B2 (en) | 2023-11-23 |
| ECSP22011156A (es) | 2022-03-31 |
| UY38860A (es) | 2021-02-26 |
| MX2022002374A (es) | 2022-03-29 |
| CR20220060A (es) | 2022-03-01 |
| WO2021038426A1 (en) | 2021-03-04 |
| EP4021572A1 (en) | 2022-07-06 |
| AU2020338971A1 (en) | 2022-01-27 |
| KR20220052934A (ko) | 2022-04-28 |
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