BR112020002351A2 - di-hidro-oxadiazinonas - Google Patents
di-hidro-oxadiazinonas Download PDFInfo
- Publication number
- BR112020002351A2 BR112020002351A2 BR112020002351-5A BR112020002351A BR112020002351A2 BR 112020002351 A2 BR112020002351 A2 BR 112020002351A2 BR 112020002351 A BR112020002351 A BR 112020002351A BR 112020002351 A2 BR112020002351 A2 BR 112020002351A2
- Authority
- BR
- Brazil
- Prior art keywords
- group
- oxadiazin
- dihydro
- trifluoromethyl
- phenyl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims abstract description 371
- 238000000034 method Methods 0.000 claims abstract description 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 23
- 201000010099 disease Diseases 0.000 claims abstract description 22
- 238000011282 treatment Methods 0.000 claims abstract description 16
- 230000003463 hyperproliferative effect Effects 0.000 claims abstract description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 6
- 238000011321 prophylaxis Methods 0.000 claims abstract description 6
- 239000004480 active ingredient Substances 0.000 claims abstract description 4
- 125000001424 substituent group Chemical group 0.000 claims description 881
- -1 atom halogen Chemical class 0.000 claims description 611
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 492
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 439
- 125000005843 halogen group Chemical group 0.000 claims description 398
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 369
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 267
- 150000003839 salts Chemical class 0.000 claims description 240
- 239000000203 mixture Substances 0.000 claims description 217
- 239000012453 solvate Substances 0.000 claims description 199
- 150000001204 N-oxides Chemical class 0.000 claims description 190
- 125000001072 heteroaryl group Chemical group 0.000 claims description 181
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 175
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims description 156
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 150
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 149
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 135
- 125000002950 monocyclic group Chemical group 0.000 claims description 128
- 125000005842 heteroatom Chemical group 0.000 claims description 100
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 95
- 125000004043 oxo group Chemical group O=* 0.000 claims description 80
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 77
- 229910052731 fluorine Chemical group 0.000 claims description 73
- 125000001153 fluoro group Chemical group F* 0.000 claims description 68
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 claims description 67
- 125000002619 bicyclic group Chemical group 0.000 claims description 66
- 125000003118 aryl group Chemical group 0.000 claims description 63
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 58
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 56
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 54
- 229910052739 hydrogen Inorganic materials 0.000 claims description 50
- 239000001257 hydrogen Substances 0.000 claims description 50
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 47
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 45
- 125000006699 (C1-C3) hydroxyalkyl group Chemical group 0.000 claims description 39
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 29
- 125000006413 ring segment Chemical group 0.000 claims description 25
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- 125000004429 atom Chemical group 0.000 claims description 22
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- 229910052763 palladium Inorganic materials 0.000 claims description 6
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- 239000003054 catalyst Substances 0.000 claims description 5
- 150000002390 heteroarenes Chemical class 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 4
- GTDKAGYSEPYXAF-UHFFFAOYSA-N 6-methyl-3,6-dihydro-1,3,4-oxadiazin-2-one Chemical compound CC1C=NNC(O1)=O GTDKAGYSEPYXAF-UHFFFAOYSA-N 0.000 claims description 4
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Classifications
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- 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
- A61K31/535—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
- A61K31/5395—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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
- C07D273/04—Six-membered 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
- C07D413/02—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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D417/10—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 carbon chain containing aromatic rings
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
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)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Catalysts (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762541627P | 2017-08-04 | 2017-08-04 | |
| US62/541,627 | 2017-08-04 | ||
| PCT/EP2018/071039 WO2019025562A1 (en) | 2017-08-04 | 2018-08-02 | DIHYDROOXADIAZINONES |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112020002351A2 true BR112020002351A2 (pt) | 2020-09-08 |
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| BR112020002351-5A BR112020002351A2 (pt) | 2017-08-04 | 2018-08-02 | di-hidro-oxadiazinonas |
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|---|---|---|---|---|
| JOP20200024A1 (ar) | 2017-08-04 | 2020-02-02 | Bayer Ag | مركبات ثنائي هيدروكساديازينون |
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