BR112019022512A2 - Compostos de heteroarila bicíclica fundida 6-6 e seu uso como inibidores de lats - Google Patents
Compostos de heteroarila bicíclica fundida 6-6 e seu uso como inibidores de lats Download PDFInfo
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- BR112019022512A2 BR112019022512A2 BR112019022512-9A BR112019022512A BR112019022512A2 BR 112019022512 A2 BR112019022512 A2 BR 112019022512A2 BR 112019022512 A BR112019022512 A BR 112019022512A BR 112019022512 A2 BR112019022512 A2 BR 112019022512A2
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- Prior art keywords
- inhibitors
- lath
- heteroaryl compounds
- present
- stereoisomer
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- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 3
- 229930186657 Lat Natural products 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
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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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- C12N5/06—Animal cells or tissues; Human cells or tissues
- C12N5/0602—Vertebrate cells
- C12N5/0618—Cells of the nervous system
- C12N5/0621—Eye cells, e.g. cornea, iris pigmented cells
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/47—Quinolines; Isoquinolines
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
- A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
- A61K35/30—Nerves; Brain; Eyes; Corneal cells; Cerebrospinal fluid; Neuronal stem cells; Neuronal precursor cells; Glial cells; Oligodendrocytes; Schwann cells; Astroglia; Astrocytes; Choroid plexus; Spinal cord tissue
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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
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- 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
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- 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
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Abstract
a presente invenção refere-se a compostos de heteroarila bicíclicos 6-6 fundidos da fórmula a2 ou a1 e seu uso como inibidores de lats, ou um sal, estereoisômero ou composição farmacêutica dos mesmos; em que as variáveis são conforme definido no presente documento (a1 e a2). a2 a1 a presente invenção refere-se adicionalmente a um método de inibição de lats em uma população de células que usa um composto de fórmula a1, ou um sal, estereoisômero ou composição farmacêutica do mesmo. a presente invenção fornece adicionalmente um método para fabricar compostos da invenção e seus usos terapêuticos. a invenção fornece adicionalmente métodos para seu preparo, para seu uso médico, para seu uso no tratamento e gerenciamento de doenças ou distúrbios.
Applications Claiming Priority (11)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762491573P | 2017-04-28 | 2017-04-28 | |
US201762491484P | 2017-04-28 | 2017-04-28 | |
US201762491475P | 2017-04-28 | 2017-04-28 | |
US201762491526P | 2017-04-28 | 2017-04-28 | |
US62/491,526 | 2017-04-28 | ||
US62/491,475 | 2017-04-28 | ||
US62/491,484 | 2017-04-28 | ||
US62/491,573 | 2017-04-28 | ||
US201862650232P | 2018-03-29 | 2018-03-29 | |
US62/650,232 | 2018-03-29 | ||
PCT/IB2018/052919 WO2018198077A2 (en) | 2017-04-28 | 2018-04-26 | 6-6 fused bicyclic heteroaryl compounds and their use as lats inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112019022512A2 true BR112019022512A2 (pt) | 2020-06-16 |
Family
ID=62148436
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112019022512-9A BR112019022512A2 (pt) | 2017-04-28 | 2018-04-26 | Compostos de heteroarila bicíclica fundida 6-6 e seu uso como inibidores de lats |
Country Status (24)
Country | Link |
---|---|
US (2) | US11458138B2 (pt) |
EP (1) | EP3615537B1 (pt) |
JP (2) | JP7247102B2 (pt) |
KR (1) | KR20190142776A (pt) |
CN (3) | CN114703144A (pt) |
AU (2) | AU2018260495B2 (pt) |
BR (1) | BR112019022512A2 (pt) |
CA (1) | CA3056906A1 (pt) |
CL (1) | CL2019003049A1 (pt) |
CO (1) | CO2019011873A2 (pt) |
CR (1) | CR20190483A (pt) |
CU (2) | CU20200080A7 (pt) |
DO (1) | DOP2019000273A (pt) |
EC (1) | ECSP19076732A (pt) |
IL (2) | IL269293B (pt) |
JO (1) | JOP20190257A1 (pt) |
MA (1) | MA49285A (pt) |
MX (1) | MX2019012756A (pt) |
PE (1) | PE20200292A1 (pt) |
PH (1) | PH12019502436A1 (pt) |
SG (1) | SG11201908615RA (pt) |
TW (1) | TW201843140A (pt) |
UY (1) | UY37703A (pt) |
WO (1) | WO2018198077A2 (pt) |
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IL295858A (en) | 2015-12-04 | 2022-10-01 | Novartis Ag | Preparations and methods for immuno-oncology |
EP3601561A2 (en) | 2017-03-22 | 2020-02-05 | Novartis AG | Compositions and methods for immunooncology |
JOP20190257A1 (ar) | 2017-04-28 | 2019-10-28 | Novartis Ag | مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats |
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TWI832871B (zh) | 2018-06-29 | 2024-02-21 | 美商英塞特公司 | Axl/mer 抑制劑之調配物 |
UY38427A (es) * | 2018-10-26 | 2020-05-29 | Novartis Ag | Métodos y composiciones para terapia con células oculares |
US20220017888A1 (en) * | 2018-12-11 | 2022-01-20 | Kyoto University | Method for inducing deletion in genomic dna |
TW202043199A (zh) | 2019-01-30 | 2020-12-01 | 日商日產化學股份有限公司 | 醯肼化合物及激酶抑制劑 |
CN112707905B (zh) * | 2019-10-25 | 2024-07-02 | 武汉誉祥医药科技有限公司 | 一种三并杂环化合物及其制备方法和用途 |
GB201915829D0 (en) * | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
GB201915831D0 (en) * | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
TW202128699A (zh) * | 2019-11-27 | 2021-08-01 | 美商建南德克公司 | 治療性化合物 |
MX2022009572A (es) | 2020-02-05 | 2022-12-13 | Univ Rockefeller | Composiciones de pirrolo[2,3-b]piridina-3-carboxamida y métodos para mejorar la pérdida de audición. |
CN111443068B (zh) * | 2020-03-06 | 2023-06-27 | 天津大学 | 具有多重刺激响应特性的纯有机室温磷光材料及筛选方法和应用 |
US20230348852A1 (en) | 2020-04-27 | 2023-11-02 | Novartis Ag | Methods and compositions for ocular cell therapy |
CN112305126A (zh) * | 2020-11-02 | 2021-02-02 | 宁夏贝利特生物科技有限公司 | 一种硝酸胍含量的测定方法 |
CN115974868B (zh) * | 2022-11-07 | 2024-04-12 | 安徽理工大学 | 一种尿嘧啶衍生物的合成方法及其抗肺纤维化方面的潜在应用 |
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EP3197557A1 (en) | 2014-09-24 | 2017-08-02 | Friedrich Miescher Institute for Biomedical Research | Lats and breast cancer |
AU2016302144B2 (en) | 2015-08-03 | 2020-10-08 | Bristol-Myers Squibb Company | Heterocyclic compounds useful as modulators of TNF alpha |
CA2996513A1 (en) | 2015-08-25 | 2018-03-02 | President And Fellows Of Harvard College | Methods and compositions relating to the diagnosis and treatment of cancer |
JOP20190257A1 (ar) | 2017-04-28 | 2019-10-28 | Novartis Ag | مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats |
UY38427A (es) * | 2018-10-26 | 2020-05-29 | Novartis Ag | Métodos y composiciones para terapia con células oculares |
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