BR112020007632A2 - composto, composição farmacêutica, método para inibir um dentre ou tanto ehmt1 quanto ehmt2, método para prevenir ou tratar um distúrbio sanguíneo, método para prevenir ou tratar um câncer e uso do composto - Google Patents
composto, composição farmacêutica, método para inibir um dentre ou tanto ehmt1 quanto ehmt2, método para prevenir ou tratar um distúrbio sanguíneo, método para prevenir ou tratar um câncer e uso do composto Download PDFInfo
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- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 description 1
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- 238000007254 oxidation reaction Methods 0.000 description 1
- LXNAVEXFUKBNMK-UHFFFAOYSA-N palladium(II) acetate Substances [Pd].CC(O)=O.CC(O)=O LXNAVEXFUKBNMK-UHFFFAOYSA-N 0.000 description 1
- YJVFFLUZDVXJQI-UHFFFAOYSA-L palladium(ii) acetate Chemical compound [Pd+2].CC([O-])=O.CC([O-])=O YJVFFLUZDVXJQI-UHFFFAOYSA-L 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 235000015320 potassium carbonate Nutrition 0.000 description 1
- 235000011181 potassium carbonates Nutrition 0.000 description 1
- 229910001414 potassium ion Inorganic materials 0.000 description 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
- 238000012746 preparative thin layer chromatography Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 201000010174 renal carcinoma Diseases 0.000 description 1
- 238000003571 reporter gene assay Methods 0.000 description 1
- 230000000754 repressing effect Effects 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 230000007727 signaling mechanism Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 235000009518 sodium iodide Nutrition 0.000 description 1
- 229910001415 sodium ion Inorganic materials 0.000 description 1
- 239000012321 sodium triacetoxyborohydride Substances 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-M sulfamate Chemical compound NS([O-])(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-M 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 150000003536 tetrazoles Chemical class 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 229940113082 thymine Drugs 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 125000002306 tributylsilyl group Chemical group C(CCC)[Si](CCCC)(CCCC)* 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
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- 239000008215 water for injection Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One 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
- C07D401/02—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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762573917P | 2017-10-18 | 2017-10-18 | |
| US62/573,917 | 2017-10-18 | ||
| PCT/US2018/056428 WO2019079540A1 (en) | 2017-10-18 | 2018-10-18 | AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS INHIBITORS OF EHMT2, SALTS THEREOF, AND METHODS OF SYNTHESIS THEREOF |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112020007632A2 true BR112020007632A2 (pt) | 2020-09-29 |
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| BR112020007632-5A BR112020007632A2 (pt) | 2017-10-18 | 2018-10-18 | composto, composição farmacêutica, método para inibir um dentre ou tanto ehmt1 quanto ehmt2, método para prevenir ou tratar um distúrbio sanguíneo, método para prevenir ou tratar um câncer e uso do composto |
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| US (2) | US20200247790A1 (enExample) |
| EP (1) | EP3697762A4 (enExample) |
| JP (2) | JP2021500334A (enExample) |
| KR (1) | KR20200101330A (enExample) |
| CN (1) | CN111417628A (enExample) |
| AU (2) | AU2018353122B2 (enExample) |
| BR (1) | BR112020007632A2 (enExample) |
| CA (1) | CA3079273A1 (enExample) |
| CL (1) | CL2020001009A1 (enExample) |
| CO (1) | CO2020005944A2 (enExample) |
| EA (1) | EA202090959A1 (enExample) |
| IL (2) | IL301746B2 (enExample) |
| MA (1) | MA50418A (enExample) |
| MX (2) | MX2020007152A (enExample) |
| SG (1) | SG11202003225YA (enExample) |
| WO (1) | WO2019079540A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110446495B (zh) | 2017-02-17 | 2023-09-05 | 特维娜有限公司 | 含有7元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法 |
| US11672800B2 (en) | 2017-04-21 | 2023-06-13 | Epizyme, Inc. | Combination therapies with EHMT2 inhibitors |
| WO2019079469A1 (en) | 2017-10-18 | 2019-04-25 | Incyte Corporation | CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| CN114249785B (zh) * | 2020-09-23 | 2024-04-05 | 常州方圆制药有限公司 | 一种2-腺苷n-吡唑的衍生物瑞加德松的制备方法 |
| JP2023546729A (ja) * | 2020-10-27 | 2023-11-07 | トレベナ・インコーポレイテッド | デルタオピオイドモジュレーターの結晶形及び非晶形 |
| WO2025240956A1 (en) * | 2024-05-17 | 2025-11-20 | Yale University | G9a/ehmt2 inhibitor use for prader-willi syndrome |
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| JP2007505858A (ja) * | 2003-09-18 | 2007-03-15 | ノバルティス アクチエンゲゼルシャフト | 増殖性障害の処置に有用な２，４−ジ（フェニルアミノ）ピリミジン |
| NZ592990A (en) * | 2005-11-01 | 2013-01-25 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| US8604042B2 (en) * | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| US9284272B2 (en) * | 2014-03-28 | 2016-03-15 | Abbvie Inc. | Inhibitors of histone methyltransferase G9a |
| ES2769648T3 (es) * | 2014-06-16 | 2020-06-26 | Fundacion Para La Investig Medica Aplicada | Nuevos compuestos como inhibidores duales de histona metiltransferasas y ADN metiltransferasasASAS |
| US20170209444A1 (en) * | 2014-06-23 | 2017-07-27 | Genentech Inc. | Methods of treating cancer and preventing cancer drug resistance |
| LT3442947T (lt) * | 2016-04-15 | 2023-09-11 | Epizyme, Inc. | Aminu pakeisti arilo arba heteroarilo junginiai, kaip ehmt1 ir ehmt2 inhibitoriai |
| TW202411220A (zh) * | 2016-12-19 | 2024-03-16 | 美商雅酶股份有限公司 | 作為ehmt2抑制劑之胺取代的雜環化合物及其使用方法 |
| AU2018243749A1 (en) * | 2017-03-31 | 2019-11-21 | Epizyme, Inc. | Methods of using EHMT2 inhibitors |
| EP3697420A4 (en) * | 2017-10-18 | 2021-11-24 | Epizyme, Inc. | METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES |
-
2018
- 2018-10-18 EA EA202090959A patent/EA202090959A1/ru unknown
- 2018-10-18 CN CN201880077022.4A patent/CN111417628A/zh active Pending
- 2018-10-18 AU AU2018353122A patent/AU2018353122B2/en active Active
- 2018-10-18 MA MA050418A patent/MA50418A/fr unknown
- 2018-10-18 US US16/756,565 patent/US20200247790A1/en not_active Abandoned
- 2018-10-18 MX MX2020007152A patent/MX2020007152A/es unknown
- 2018-10-18 CA CA3079273A patent/CA3079273A1/en active Pending
- 2018-10-18 BR BR112020007632-5A patent/BR112020007632A2/pt unknown
- 2018-10-18 WO PCT/US2018/056428 patent/WO2019079540A1/en not_active Ceased
- 2018-10-18 SG SG11202003225YA patent/SG11202003225YA/en unknown
- 2018-10-18 JP JP2020521599A patent/JP2021500334A/ja not_active Withdrawn
- 2018-10-18 KR KR1020207013781A patent/KR20200101330A/ko not_active Ceased
- 2018-10-18 IL IL301746A patent/IL301746B2/en unknown
- 2018-10-18 EP EP18869308.9A patent/EP3697762A4/en not_active Withdrawn
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2020
- 2020-04-15 CL CL2020001009A patent/CL2020001009A1/es unknown
- 2020-04-16 IL IL273974A patent/IL273974B2/en unknown
- 2020-05-15 CO CONC2020/0005944A patent/CO2020005944A2/es unknown
- 2020-07-13 MX MX2024012124A patent/MX2024012124A/es unknown
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2022
- 2022-03-24 US US17/703,155 patent/US20220324851A1/en not_active Abandoned
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2023
- 2023-01-11 JP JP2023002371A patent/JP2023036991A/ja active Pending
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2024
- 2024-02-22 AU AU2024201165A patent/AU2024201165A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20220324851A1 (en) | 2022-10-13 |
| IL301746B1 (en) | 2024-09-01 |
| SG11202003225YA (en) | 2020-05-28 |
| AU2018353122B2 (en) | 2023-11-23 |
| CA3079273A1 (en) | 2019-04-25 |
| CL2020001009A1 (es) | 2020-12-18 |
| EA202090959A1 (ru) | 2020-07-13 |
| MX2024012124A (es) | 2025-02-10 |
| IL273974B2 (en) | 2023-08-01 |
| KR20200101330A (ko) | 2020-08-27 |
| EP3697762A4 (en) | 2021-04-07 |
| IL301746B2 (en) | 2025-01-01 |
| MA50418A (fr) | 2021-04-07 |
| CO2020005944A2 (es) | 2020-07-31 |
| JP2021500334A (ja) | 2021-01-07 |
| IL273974B1 (en) | 2023-04-01 |
| MX2020007152A (es) | 2020-12-10 |
| WO2019079540A1 (en) | 2019-04-25 |
| US20200247790A1 (en) | 2020-08-06 |
| AU2024201165A1 (en) | 2024-03-14 |
| IL301746A (en) | 2023-05-01 |
| IL273974A (en) | 2020-05-31 |
| JP2023036991A (ja) | 2023-03-14 |
| EP3697762A1 (en) | 2020-08-26 |
| AU2018353122A1 (en) | 2020-06-04 |
| CN111417628A (zh) | 2020-07-14 |
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