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 lats

Info

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
compounds
lats
fused
Prior art date
Application number
CR20190483A
Other languages
English (en)
Inventor
Timothy Hoffmann
Jun Liu
Tingting Mo
Jiangfeng Pan
Yefen Zou
Dirk Behnke
Xueshi Hao
Juergen Klaus Maibaum
Frada Berenshteyn
Arnaud Lacoste
Cameron Lee
Yahu Liu
Yun Feng Xie
Shanshan Yan
Qihui Jin
Jan Tchorz
Xin Qu
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CR20190483A publication Critical patent/CR20190483A/es

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • 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
    • C12N15/8645—Adeno-associated virus
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • 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 [CRISPR]
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2501/00—Active agents used in cell culture processes, e.g. differentation
    • C12N2501/70—Enzymes
    • C12N2501/72—Transferases [EC 2.]
    • C12N2501/727—Kinases (EC 2.7.)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2502/00—Coculture with; Conditioned medium produced by
    • C12N2502/13—Coculture with; Conditioned medium produced by connective tissue cells; generic mesenchyme cells, e.g. so-called "embryonic fibroblasts"
    • C12N2502/1352—Mesenchymal stem cells
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2502/00—Coculture with; Conditioned medium produced by
    • C12N2502/27—Lung cells, respiratory tract cells
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2510/00—Genetically modified cells

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Plant Pathology (AREA)
  • Developmental Biology & Embryology (AREA)
  • Virology (AREA)
  • Physics & Mathematics (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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.
CR20190483A 2017-04-28 2018-04-26 Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats CR20190483A (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201762491526P 2017-04-28 2017-04-28
US201762491475P 2017-04-28 2017-04-28
US201762491484P 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 (25)

Country Link
US (2) US11458138B2 (es)
EP (1) EP3615537B1 (es)
JP (2) JP7247102B2 (es)
KR (1) KR20190142776A (es)
CN (3) CN114703144A (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)
ES (1) ES2983611T3 (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 (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108699557B (zh) 2015-12-04 2025-08-15 诺华股份有限公司 用于免疫肿瘤学的组合物和方法
CN114456176B (zh) 2016-03-28 2024-08-30 因赛特公司 作为tam抑制剂的吡咯并三嗪化合物
KR20190130608A (ko) 2017-03-22 2019-11-22 노파르티스 아게 면역종양학을 위한 조성물 및 방법
JOP20190257A1 (ar) 2017-04-28 2019-10-28 Novartis Ag مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats
KR102739325B1 (ko) 2017-09-27 2024-12-09 인사이트 코포레이션 Tam 억제제로서 유용한 피롤로트리아진 유도체의 염
EP3804707A4 (en) 2018-06-08 2022-03-16 Nissan Chemical Corporation KINASE INHIBITOR
US11241438B2 (en) 2018-06-29 2022-02-08 Incyte Corporation Formulations of an AXL/MER inhibitor
CA3115998A1 (en) * 2018-10-16 2020-04-23 The Schepens Eye Research Institute, Inc. Bioadhesive for soft tissue repair
UY38427A (es) * 2018-10-26 2020-05-29 Novartis Ag Métodos y composiciones para terapia con células oculares
EP3896158A4 (en) * 2018-12-11 2022-11-02 Kyoto University METHODS OF INDUCING A 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
WO2021108483A1 (en) * 2019-11-27 2021-06-03 Genentech, Inc. Therapeutic compounds
US12617785B2 (en) * 2020-02-05 2026-05-05 The Rockefeller University Pyrrolo[2,3-b]pyridine-3-carboxamide compositions and methods for ameliorating hearing loss
PH12022552347A1 (en) 2020-03-06 2024-01-29 Incyte Corp Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
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
PE20230845A1 (es) * 2020-04-28 2023-05-23 Global Blood Therapeutics Inc Pirimidinas cicloalquiladas como inhibidores de la ferroportina
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
AU2022284188A1 (en) * 2021-06-04 2023-11-30 Genentech, Inc. 2, 8-diazaspiro [4.5] decane compounds
CN117795330A (zh) * 2021-08-23 2024-03-29 Emd密理博公司 用于光聚合电泳凝胶的系统和方法
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
WO2024211621A1 (en) * 2023-04-04 2024-10-10 Children's Hospital Los Angeles Lats kinase inhibitor to treat retinal degeneration
CN119462609B (zh) * 2024-10-25 2025-12-26 烟台皓元生物医药科技有限公司 一种lats抑制剂vt02956的制备方法

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004065392A1 (en) 2003-01-24 2004-08-05 Smithkline Beecham Corporation Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands
EP1871377A1 (en) 2005-02-25 2008-01-02 Kudos Pharmaceuticals Ltd 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors
WO2008122614A1 (en) 2007-04-06 2008-10-16 Novartis Ag 2, 6-naphthyridine derivatives as protein kinase modulators
EP2318377B1 (en) 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
US20110319409A1 (en) * 2010-06-23 2011-12-29 Cox Christopher D 7-aza-quinazoline pde10 inhibitors
US9347041B2 (en) * 2011-07-15 2016-05-24 Osaka University Method for preparing corneal endothelial cell
CA2845191A1 (en) 2011-09-27 2013-04-04 F. Hoffmann-La Roche Ag Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
EA030253B1 (ru) * 2012-09-28 2018-07-31 Кэнсэр Ресерч Текнолоджи Лимитед Азахиназолиновые ингибиторы атипичной протеинкиназы c
CN111206032B (zh) * 2013-12-12 2024-07-19 布罗德研究所有限公司 用于基因组编辑的crispr-cas系统和组合物的递送、用途和治疗应用
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
EP3197557A1 (en) 2014-09-24 2017-08-02 Friedrich Miescher Institute for Biomedical Research Lats and breast cancer
TW201718536A (zh) 2015-08-03 2017-06-01 必治妥美雅史谷比公司 可作為ＴＮＦα調節劑之雜環化合物
US20200216906A1 (en) 2015-08-25 2020-07-09 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

Also Published As

Publication number Publication date
CA3056906A1 (en) 2018-11-01
RU2019138304A3 (es) 2021-07-13
JP2022188056A (ja) 2022-12-20
WO2018198077A3 (en) 2019-02-14
DOP2019000273A (es) 2019-12-15
EP3615537A2 (en) 2020-03-04
CN114621222B (zh) 2024-12-17
SG11201908615RA (en) 2019-11-28
WO2018198077A2 (en) 2018-11-01
CN110573511B (zh) 2023-04-25
US20180344738A1 (en) 2018-12-06
ES2983611T3 (es) 2024-10-23
CL2019003049A1 (es) 2020-02-07
ECSP19076732A (es) 2019-10-31
MA49285A (fr) 2020-03-04
JOP20190257A1 (ar) 2019-10-28
CU20190086A7 (es) 2020-11-30
AU2021286281A1 (en) 2022-01-06
CO2019011873A2 (es) 2020-01-17
EP3615537B1 (en) 2024-03-06
KR20190142776A (ko) 2019-12-27
JP2020517698A (ja) 2020-06-18
CN110573511A (zh) 2019-12-13
CN114703144A (zh) 2022-07-05
JP7247102B2 (ja) 2023-03-28
UY37703A (es) 2018-11-30
MX2019012756A (es) 2019-12-16
AU2018260495B2 (en) 2021-09-16
TW201843140A (zh) 2018-12-16
PH12019502436A1 (en) 2020-07-20
PE20200292A1 (es) 2020-02-05
IL292857A (en) 2022-07-01
CU20200080A7 (es) 2021-05-12
US20230190751A1 (en) 2023-06-22
IL269293B (en) 2022-06-01
IL269293A (en) 2019-11-28
CN114621222A (zh) 2022-06-14
RU2019138304A (ru) 2021-05-28
AU2018260495A1 (en) 2019-10-17
BR112019022512A2 (pt) 2020-06-16
US11458138B2 (en) 2022-10-04

Similar Documents

Publication Publication Date Title
ECSP19076732A (es) Compuestos de heteroarilo bicíclicos 6–6 fusionados y su uso como inhibidores de lats
MX2022015272A (es) Inhibidores de la proteina kras g12c y usos de estos.
CL2018001145A1 (es) Compuestos inhibidores de jak quinasa para el tratamiento de enfermedad respiratoria
BR112021025964A2 (pt) Formas de sal de ácido bempedoico e métodos para uso das mesmas
CO2021002976A2 (es) Amidas heterocíclicas de 5 a 7 miembros como inhibidores de jak
JOP20190151B1 (ar) مركبات أمينو - ترايازولو بيريدين واستخدامها في علاج سرطان
CO2021002977A2 (es) Dimetilaminoazetidinaminas como inhibidores de jak
DOP2016000281A (es) Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso para tratar cáncer
PE20180258A1 (es) Inhibidores de bromodominio
CO2017012267A2 (es) Compuestos de naftiridina como inhibidores de la quinasa jak
MX382671B (es) Compuestos para usarse en el tratamiento o mejoramiento de la enfermedad de huntington
UY37379A (es) Derivados de n-(piridin-2-il)piridina-sulfonamida y su uso en el tratamiento de enfermedades
CR20200334A (es) Compuestos, composiciones y métodos para tratar enfermedades que involucren tejidos con enfermedades ácidas o hipóxicas
MX2019010541A (es) Compuestos de imidazo-piperidina fusionada como inhibidores de jak.
UY36207A (es) Inhibidores de la syk
CL2018001569A1 (es) Compuestos heteroaromáticos como inhibidores de btk
BR112016011065A8 (pt) composto cristalino, composição farmacêutica, forma de dosagem, método para tratar anemia
MX391156B (es) Forma polimorfica de sepiapterina.
DOP2016000308A (es) Compuestos de 1, 3, 4-tiadiazol y uso de los mismos para el tratamiento del cáncer
MX2021010122A (es) Compuestos de imidazopiridinilo y su uso para el tratamiento de trastornos neurodegenerativos.
CL2021001198A1 (es) Compuestos heteroaromáticos como inhibidores de vanina
CO2017003305A2 (es) Derivados de la amida del ácido 2-[piridin-3-il]-2,3-dihidro-benzo[1,4]dioxin-5-carboxílico o del 2-[piridin-3-il]-2,3-dihidro-benzo[1,4]dioxin-5-carbonitrilo como inhibidores de aldosterona sintasa
BR112023018237A2 (pt) Fenalquilaminas e métodos para fabricação e uso das mesmas
DOP2019000100A (es) Derivados de naftiridinona y su uso en el tratamiento de la arritmia
UY39181A (es) COMPUESTOS Y COMPOSICIONES PARA INHIBIR LA ACTIVIDAD DE HIF2a Y SUS MÉTODOS DE USO