CR20190483A - Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats - Google Patents
Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de latsInfo
- Publication number
- CR20190483A CR20190483A CR20190483A CR20190483A CR20190483A CR 20190483 A CR20190483 A CR 20190483A CR 20190483 A CR20190483 A CR 20190483A CR 20190483 A CR20190483 A CR 20190483A CR 20190483 A CR20190483 A CR 20190483A
- Authority
- CR
- Costa Rica
- Prior art keywords
- present
- invention further
- lats
- compounds
- bicyclic heteroaryl
- Prior art date
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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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- C—CHEMISTRY; METALLURGY
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- C12N5/00—Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
- 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
- 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
- A61K31/4353—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
- 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
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/70503—Immunoglobulin superfamily
- C07K14/70539—MHC-molecules, e.g. HLA-molecules
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/52—Genes encoding for enzymes or proenzymes
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/63—Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- C12N15/79—Vectors or expression systems specially adapted for eukaryotic hosts
- C12N15/85—Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
- C12N15/86—Viral vectors
- C12N15/864—Parvoviral vectors, e.g. parvovirus, densovirus
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/20—Type of nucleic acid involving clustered regularly interspaced short palindromic repeats [CRISPRs]
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- C12N2501/70—Enzymes
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- C12N2502/00—Coculture with; Conditioned medium produced by
- C12N2502/08—Coculture with; Conditioned medium produced by cells of the nervous system
- C12N2502/085—Coculture with; Conditioned medium produced by cells of the nervous system eye cells
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- C12N2502/13—Coculture with; Conditioned medium produced by connective tissue cells; generic mesenchyme cells, e.g. so-called "embryonic fibroblasts"
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Abstract
La presente invención se refiere a compuestos de heteroarilo bicíclicos 6¿6 fusionados de la Fórmula A2 o A1 y su uso como inhibidores de LATS, o una sal, un estereoisómero o una composición farmacéutica de dichos compuestos; donde las variables son como se definen en el presente documento (A1 & A2). La presente invención se refiere además a un método de inhibición de LATS en una población de células, usando un compuesto de Fórmula A1, o una sal, un estereoisómero o una composición farmacéutica de dicho compuesto. La presente invención proporciona además un método para fabricar compuestos de la invención y sus usos terapéuticos. La invención proporciona adicionalmente métodos para su preparación, para su uso médico, su uso en el tratamiento y el abordaje de enfermedades o trastornos.The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein (A1 & A2). The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762491484P | 2017-04-28 | 2017-04-28 | |
US201762491526P | 2017-04-28 | 2017-04-28 | |
US201762491475P | 2017-04-28 | 2017-04-28 | |
US201762491573P | 2017-04-28 | 2017-04-28 | |
US201862650232P | 2018-03-29 | 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 |
---|---|
CR20190483A true CR20190483A (es) | 2019-11-20 |
Family
ID=62148436
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20190483A CR20190483A (es) | 2017-04-28 | 2018-04-26 | Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats |
Country Status (24)
Country | Link |
---|---|
US (2) | US11458138B2 (es) |
EP (1) | EP3615537B1 (es) |
JP (2) | JP7247102B2 (es) |
KR (1) | KR20190142776A (es) |
CN (3) | CN110573511B (es) |
AU (2) | AU2018260495B2 (es) |
BR (1) | BR112019022512A2 (es) |
CA (1) | CA3056906A1 (es) |
CL (1) | CL2019003049A1 (es) |
CO (1) | CO2019011873A2 (es) |
CR (1) | CR20190483A (es) |
CU (2) | CU20200080A7 (es) |
DO (1) | DOP2019000273A (es) |
EC (1) | ECSP19076732A (es) |
IL (2) | IL269293B (es) |
JO (1) | JOP20190257A1 (es) |
MA (1) | MA49285A (es) |
MX (1) | MX2019012756A (es) |
PE (1) | PE20200292A1 (es) |
PH (1) | PH12019502436A1 (es) |
SG (1) | SG11201908615RA (es) |
TW (1) | TW201843140A (es) |
UY (1) | UY37703A (es) |
WO (1) | WO2018198077A2 (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2018237159A1 (en) | 2017-03-22 | 2019-09-05 | Intellia Therapeutics, Inc. | 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 |
WO2019235569A1 (ja) | 2018-06-08 | 2019-12-12 | 日産化学株式会社 | キナーゼ阻害剤 |
JP2021529765A (ja) | 2018-06-29 | 2021-11-04 | インサイト・コーポレイションIncyte Corporation | Axl/mer阻害剤の製剤 |
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 |
WO2020158841A1 (ja) | 2019-01-30 | 2020-08-06 | 日産化学株式会社 | ヒドラジド化合物及びキナーゼ阻害剤 |
CN112707905A (zh) * | 2019-10-25 | 2021-04-27 | 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 |
JP2023503970A (ja) * | 2019-11-27 | 2023-02-01 | ジェネンテック, インコーポレイテッド | 治療用化合物 |
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 |
JP2023522784A (ja) | 2020-04-27 | 2023-05-31 | ノバルティス アーゲー | 眼細胞療法のための方法及び組成物 |
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 |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2004065392A1 (en) | 2003-01-24 | 2004-08-05 | Smithkline Beecham Corporation | Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands |
MX2007010401A (es) | 2005-02-25 | 2008-02-19 | Kudos Pharm Ltd | Derivados de 2,4-diamino-piridopirimidina y su uso como inhbidores de mtor. |
CA2682339A1 (en) * | 2007-04-06 | 2008-10-16 | Novartis Ag | 2 , 6-naphthyridine derivatives as protein kinase modulators |
RU2473549C2 (ru) | 2008-07-31 | 2013-01-27 | Дженентек, Инк. | Пиримидиновые соединения, композиции и способы применения |
US20110319409A1 (en) * | 2010-06-23 | 2011-12-29 | Cox Christopher D | 7-aza-quinazoline pde10 inhibitors |
JP5761827B2 (ja) * | 2011-07-15 | 2015-08-12 | 国立大学法人大阪大学 | 角膜内皮細胞の調製方法 |
WO2013045461A1 (en) | 2011-09-27 | 2013-04-04 | F. Hoffmann-La Roche Ag | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
SG11201502301YA (en) | 2012-09-28 | 2015-04-29 | Cancer Rec Tech Ltd | Azaquinazoline inhibitors of atypical protein kinase c |
AU2014361781B2 (en) * | 2013-12-12 | 2021-04-01 | Massachusetts Institute Of Technology | Delivery, use and therapeutic applications of the CRISPR -Cas systems and compositions for genome editing |
TWI675836B (zh) * | 2014-03-25 | 2019-11-01 | 美商伊格尼塔公司 | 非典型蛋白質激酶c之氮雜喹唑啉抑制劑 |
WO2016046768A1 (en) | 2014-09-24 | 2016-03-31 | Friedrich Miescher Institute For Biomedical Research | Lats and breast cancer |
MA43512A (fr) | 2015-08-03 | 2018-11-07 | Bristol Myers Squibb Co | Composés hétérocycliques utiles en tant que modulateurs du tnf alpha |
WO2017035116A1 (en) | 2015-08-25 | 2017-03-02 | 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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2017
- 2017-06-16 JO JOP/2019/0257A patent/JOP20190257A1/ar unknown
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2018
- 2018-04-26 SG SG11201908615R patent/SG11201908615RA/en unknown
- 2018-04-26 MA MA049285A patent/MA49285A/fr unknown
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