CU20190086A7 - Compuestos de heteroarilo bicíclicos 6-6 fusionados útiles como inhibidores de lats - Google Patents
Compuestos de heteroarilo bicíclicos 6-6 fusionados útiles como inhibidores de latsInfo
- Publication number
- CU20190086A7 CU20190086A7 CU2019000086A CU20190086A CU20190086A7 CU 20190086 A7 CU20190086 A7 CU 20190086A7 CU 2019000086 A CU2019000086 A CU 2019000086A CU 20190086 A CU20190086 A CU 20190086A CU 20190086 A7 CU20190086 A7 CU 20190086A7
- Authority
- CU
- Cuba
- Prior art keywords
- bicyclic heteroaryl
- compounds useful
- heteroaryl compounds
- fused bicyclic
- lats
- Prior art date
Links
Classifications
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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
-
- 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
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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
- 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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- 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
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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
-
- 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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- 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
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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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
- C12N15/8645—Adeno-associated virus
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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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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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- 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.)
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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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- C12N2502/00—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
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- C12N2502/00—Coculture with; Conditioned medium produced by
- C12N2502/27—Lung cells, respiratory tract cells
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- C12N2510/00—Genetically modified cells
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- 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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
- Cell Biology (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
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- Physics & Mathematics (AREA)
- Developmental Biology & Embryology (AREA)
- Immunology (AREA)
- Toxicology (AREA)
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- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
<p>La presente invención se refiere a compuestos de heteroarilo bicíclicos 6-6 fusionados de la Fórmula A2 o A1 para utilizar como inhibidores de LATS, o una sal, un estereoisómero a o una composición farmacéutica de dichos compuestos; donde las variables son como se definen en el presente documento (A1 & A2).</p> <p>ESPACIO PARA LAS FÓRMULAS</p> <p>La presente invención se refiere además a un método de inhibición de LATS en una población de células, usando un compuesto de Formula A1, o una sal, un estereoisómero o una composición farmacéutica de dicho compuesto. La presente invención proporciona además un método para preparar y fabricar compuestos de la invención.</p>
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762491526P | 2017-04-28 | 2017-04-28 | |
US201762491573P | 2017-04-28 | 2017-04-28 | |
US201762491475P | 2017-04-28 | 2017-04-28 | |
US201762491484P | 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 |
---|---|
CU20190086A7 true CU20190086A7 (es) | 2020-11-30 |
Family
ID=62148436
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CU2019000086A CU20190086A7 (es) | 2017-04-28 | 2018-04-26 | Compuestos de heteroarilo bicíclicos 6-6 fusionados útiles como inhibidores de lats |
CU2020000080A CU20200080A7 (es) | 2017-04-28 | 2018-04-26 | Kit que comprende un inhibidor de lats para el suministro ocular |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CU2020000080A CU20200080A7 (es) | 2017-04-28 | 2018-04-26 | Kit que comprende un inhibidor de lats para el suministro ocular |
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) | CU20190086A7 (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 |
---|---|---|---|---|
US11851659B2 (en) | 2017-03-22 | 2023-12-26 | 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 |
JPWO2019235569A1 (ja) | 2018-06-08 | 2021-07-08 | 日産化学株式会社 | キナーゼ阻害剤 |
CN117771250A (zh) | 2018-06-29 | 2024-03-29 | 因赛特公司 | Axl/mer抑制剂的制剂 |
UY38427A (es) | 2018-10-26 | 2020-05-29 | Novartis Ag | Métodos y composiciones para terapia con células oculares |
WO2020122104A1 (ja) * | 2018-12-11 | 2020-06-18 | 国立大学法人京都大学 | ゲノムdnaに欠失を誘導する方法 |
EP3915636A4 (en) | 2019-01-30 | 2022-03-09 | Nissan Chemical Corporation | HYDRAZIDE COMPOUND AND KINASE INHIBITOR |
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 |
EP4065230A1 (en) * | 2019-11-27 | 2022-10-05 | Genentech, Inc. | Therapeutic compounds |
AU2021215925A1 (en) * | 2020-02-05 | 2022-09-08 | The Rockefeller University | Pyrrolo [2,3-b]pyridine-3-carboxamide compositions and methods for ameliorating hearing loss |
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 |
EP4142879A1 (en) | 2020-04-27 | 2023-03-08 | 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 |
Family Cites Families (15)
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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 |
KR20070113252A (ko) | 2005-02-25 | 2007-11-28 | 쿠도스 파마슈티칼스 리미티드 | 2,4-디아미노-피리도피리미딘 유도체 및 이의 mTOR억제제로서의 용도 |
EP2144908A1 (en) * | 2007-04-06 | 2010-01-20 | 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 |
EP2733201B1 (en) * | 2011-07-15 | 2018-02-21 | Osaka University | Method for preparing corneal endothelial cell |
JP6120861B2 (ja) | 2011-09-27 | 2017-04-26 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ピラゾール−4−イル−ヘテロシクリル−カルボキサミド化合物と使用方法 |
TWI663165B (zh) * | 2012-09-28 | 2019-06-21 | 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 |
BR112016013201B1 (pt) * | 2013-12-12 | 2023-01-31 | The Broad Institute, Inc. | Uso de uma composição compreendendo um sistema crispr-cas no tratamento de uma doença genética ocular |
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 |
US10865191B2 (en) | 2015-08-03 | 2020-12-15 | Bristol-Myers Squibb Company | Heterocyclic compounds useful as modulators of TNF alpha |
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 |
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2017
- 2017-06-16 JO JOP/2019/0257A patent/JOP20190257A1/ar unknown
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2018
- 2018-04-26 AU AU2018260495A patent/AU2018260495B2/en active Active
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