BR112018075992A2 - piridinas substituídas como inibidores da dnmt1 - Google Patents
piridinas substituídas como inibidores da dnmt1Info
- Publication number
- BR112018075992A2 BR112018075992A2 BR112018075992A BR112018075992A BR112018075992A2 BR 112018075992 A2 BR112018075992 A2 BR 112018075992A2 BR 112018075992 A BR112018075992 A BR 112018075992A BR 112018075992 A BR112018075992 A BR 112018075992A BR 112018075992 A2 BR112018075992 A2 BR 112018075992A2
- Authority
- BR
- Brazil
- Prior art keywords
- dnmt1
- relates
- compound
- iar
- sickle cell
- Prior art date
Links
Classifications
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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
- A61K31/435—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
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D213/60—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- 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
- C07D213/60—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
a invenção refere-se a derivados substituídos da piridina mais especificamente, a invenção refere-se a compostos de acordo com a fórmula (iar): (iar) em que yar, x1ar, x2ar, r1ar, r2ar, r3ar, r4ar e r5ar são conforme definidos neste documento; ou um sal ou pró-fármaco farmaceuticamente aceitável dos mesmos. os compostos da invenção são inibidores seletivos da dnmt1 e podem ser úteis no tratamento contra o câncer, síndromes pré-cancerosas, transtornos beta-hemoglobinopatia, doença das células falciformes, anemia de células falciformes e beta-talassemia, além de outras doenças associadas à inibição da dnmt1. logo, a invenção também se refere a composições farmacêuticas que compreendem um composto da invenção. ademais, a invenção também se refere a métodos para inibir a atividade da dnmt1 e ao tratamento de transtornos associados a esta usando um composto da invenção ou uma composição farmacêutica compreendendo um composto da invenção.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662349227P | 2016-06-13 | 2016-06-13 | |
US201662393256P | 2016-09-12 | 2016-09-12 | |
US201662412343P | 2016-10-25 | 2016-10-25 | |
PCT/IB2017/053511 WO2017216727A1 (en) | 2016-06-13 | 2017-06-13 | Substituted pyridines as inhibitors of dnmt1 |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112018075992A2 true BR112018075992A2 (pt) | 2019-04-02 |
Family
ID=59239935
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018075992A BR112018075992A2 (pt) | 2016-06-13 | 2017-06-13 | piridinas substituídas como inibidores da dnmt1 |
Country Status (20)
Country | Link |
---|---|
US (1) | US10975056B2 (pt) |
EP (1) | EP3468953B1 (pt) |
JP (1) | JP7051829B2 (pt) |
KR (1) | KR20190017030A (pt) |
CN (1) | CN109563043B (pt) |
AU (1) | AU2017283790B2 (pt) |
BR (1) | BR112018075992A2 (pt) |
CA (2) | CA3026226A1 (pt) |
CL (1) | CL2018003577A1 (pt) |
CO (1) | CO2018013717A2 (pt) |
CR (1) | CR20180580A (pt) |
DO (1) | DOP2018000273A (pt) |
IL (1) | IL263163B (pt) |
JO (1) | JOP20180120A1 (pt) |
MA (1) | MA45244A (pt) |
MX (1) | MX2018015483A (pt) |
PE (1) | PE20190971A1 (pt) |
PH (1) | PH12018502633A1 (pt) |
SG (1) | SG11201809559UA (pt) |
WO (2) | WO2017216727A1 (pt) |
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BR112019006816A8 (pt) | 2016-10-04 | 2023-02-07 | Merck Sharp & Dohme | Compostos de benzo[b]tiofeno como agonistas de sting, composição farmacêutica e uso dos mesmos |
ES2927019T3 (es) | 2017-03-28 | 2022-11-02 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de enfermedades hepáticas |
US11466047B2 (en) | 2017-05-12 | 2022-10-11 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
MA49772A (fr) | 2017-08-04 | 2021-04-21 | Merck Sharp & Dohme | Agonistes benzo[b]thiophène de sting pour le traitement du cancer |
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WO2015110999A1 (en) | 2014-01-24 | 2015-07-30 | Piramal Enterprises Limited | Ezh2 inhibitors and uses thereof |
-
2017
- 2017-06-13 PE PE2018003216A patent/PE20190971A1/es unknown
- 2017-06-13 CR CR20180580A patent/CR20180580A/es unknown
- 2017-06-13 CA CA3026226A patent/CA3026226A1/en not_active Abandoned
- 2017-06-13 BR BR112018075992A patent/BR112018075992A2/pt active Search and Examination
- 2017-06-13 MX MX2018015483A patent/MX2018015483A/es unknown
- 2017-06-13 SG SG11201809559UA patent/SG11201809559UA/en unknown
- 2017-06-13 CA CA3026211A patent/CA3026211A1/en active Pending
- 2017-06-13 WO PCT/IB2017/053511 patent/WO2017216727A1/en unknown
- 2017-06-13 CN CN201780036908.XA patent/CN109563043B/zh active Active
- 2017-06-13 JP JP2019517187A patent/JP7051829B2/ja active Active
- 2017-06-13 WO PCT/IB2017/053509 patent/WO2017216726A1/en active Application Filing
- 2017-06-13 US US16/309,121 patent/US10975056B2/en active Active
- 2017-06-13 AU AU2017283790A patent/AU2017283790B2/en not_active Ceased
- 2017-06-13 EP EP17733902.5A patent/EP3468953B1/en active Active
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- 2017-06-13 KR KR1020197000766A patent/KR20190017030A/ko not_active Application Discontinuation
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- 2018-12-10 JO JOP/2018/0120A patent/JOP20180120A1/ar unknown
- 2018-12-12 CL CL2018003577A patent/CL2018003577A1/es unknown
- 2018-12-13 PH PH12018502633A patent/PH12018502633A1/en unknown
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MA45244A (fr) | 2019-04-17 |
CR20180580A (es) | 2019-07-02 |
PH12018502633A1 (en) | 2019-09-30 |
CA3026226A1 (en) | 2017-12-21 |
IL263163A (en) | 2018-12-31 |
MX2018015483A (es) | 2019-03-18 |
EP3468953A1 (en) | 2019-04-17 |
JP2019517596A (ja) | 2019-06-24 |
WO2017216727A1 (en) | 2017-12-21 |
EP3468953B1 (en) | 2024-05-22 |
AU2017283790A1 (en) | 2018-11-22 |
AU2017283790B2 (en) | 2019-08-29 |
JP7051829B2 (ja) | 2022-04-11 |
KR20190017030A (ko) | 2019-02-19 |
US10975056B2 (en) | 2021-04-13 |
CA3026211A1 (en) | 2017-12-21 |
US20190194166A1 (en) | 2019-06-27 |
PE20190971A1 (es) | 2019-07-09 |
DOP2018000273A (es) | 2019-03-31 |
SG11201809559UA (en) | 2018-12-28 |
CL2018003577A1 (es) | 2019-04-05 |
CO2018013717A2 (es) | 2019-01-18 |
WO2017216726A1 (en) | 2017-12-21 |
CN109563043A (zh) | 2019-04-02 |
IL263163B (en) | 2021-10-31 |
CN109563043B (zh) | 2022-05-31 |
JOP20180120A1 (ar) | 2019-01-30 |
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