JOP20190257A1 - مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats - Google Patents
مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات latsInfo
- Publication number
- JOP20190257A1 JOP20190257A1 JOP/2019/0257A JOP20190257A JOP20190257A1 JO P20190257 A1 JOP20190257 A1 JO P20190257A1 JO P20190257 A JOP20190257 A JO P20190257A JO P20190257 A1 JOP20190257 A1 JO P20190257A1
- Authority
- JO
- Jordan
- Prior art keywords
- bicyclic heteroaryl
- fused bicyclic
- heteroaryl compounds
- present
- lats
- Prior art date
Links
- 229930186657 Lat Natural products 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000003202 long acting thyroid stimulator Substances 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
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
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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
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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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- 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
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- A—HUMAN NECESSITIES
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- 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
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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
- C07D487/04—Ortho-condensed systems
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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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- C12N15/09—Recombinant DNA-technology
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- C12N15/52—Genes encoding for enzymes or proenzymes
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- C12N15/09—Recombinant DNA-technology
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Abstract
يتعلق الاختراع الحالي بمركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 بالصيغة A2 أو A1 واستخدامها كمثبطات LATS، أو ملح، أيزومر فراغي أو تركيبة صيدلانية منها؛ حيث تكون المتغيرات كما تم تعريفها في هذه الوثيقة. يتعلق الاختراع الحالي أيضاً بطريقة لتثبيط LATS في مجموعة خلايا باستخدام مركب بالصيغة A1، أو ملح، أيزومر فراغي أو تركيبة صيدلانية منها. يقدم الاختراع الحالي أيضاً طريقة لتصنيع مركبات الاختراع، واستخداماتها العلاجية. يقدم الاختراع أيضاً طرق لتحضيرها، واستخدامها الطبي، واستخدامها في معالجة وإدارة الأمراض أو الاضطرابات. الشكل 1 و صور A1, A2
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762491484P | 2017-04-28 | 2017-04-28 | |
US201762491573P | 2017-04-28 | 2017-04-28 | |
US201762491475P | 2017-04-28 | 2017-04-28 | |
US201762491526P | 2017-04-28 | 2017-04-28 | |
US201862650232P | 2018-03-29 | 2018-03-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
JOP20190257A1 true JOP20190257A1 (ar) | 2019-10-28 |
Family
ID=62148436
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JOP/2019/0257A JOP20190257A1 (ar) | 2017-04-28 | 2017-06-16 | مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats |
Country Status (25)
Country | Link |
---|---|
US (2) | US11458138B2 (ar) |
EP (1) | EP3615537B1 (ar) |
JP (2) | JP7247102B2 (ar) |
KR (1) | KR20190142776A (ar) |
CN (3) | CN114703144A (ar) |
AU (2) | AU2018260495B2 (ar) |
BR (1) | BR112019022512A2 (ar) |
CA (1) | CA3056906A1 (ar) |
CL (1) | CL2019003049A1 (ar) |
CO (1) | CO2019011873A2 (ar) |
CR (1) | CR20190483A (ar) |
CU (2) | CU20200080A7 (ar) |
DO (1) | DOP2019000273A (ar) |
EC (1) | ECSP19076732A (ar) |
ES (1) | ES2983611T3 (ar) |
IL (2) | IL269293B (ar) |
JO (1) | JOP20190257A1 (ar) |
MA (1) | MA49285A (ar) |
MX (1) | MX2019012756A (ar) |
PE (1) | PE20200292A1 (ar) |
PH (1) | PH12019502436A1 (ar) |
SG (1) | SG11201908615RA (ar) |
TW (1) | TW201843140A (ar) |
UY (1) | UY37703A (ar) |
WO (1) | WO2018198077A2 (ar) |
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UA126373C2 (uk) | 2015-12-04 | 2022-09-28 | Новартіс Аг | Композиція і спосіб для імуноонкології |
CA3054621A1 (en) | 2017-03-22 | 2018-09-27 | 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 |
LT3687996T (lt) | 2017-09-27 | 2022-01-10 | Incyte Corporation | Pirolotriazino darinių druskos, naudingos kaip tam inhibitoriai |
WO2019235569A1 (ja) | 2018-06-08 | 2019-12-12 | 日産化学株式会社 | キナーゼ阻害剤 |
SG11202013163TA (en) | 2018-06-29 | 2021-01-28 | Incyte Corp | Formulations of an axl/mer inhibitor |
WO2020081673A1 (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 |
US20220017888A1 (en) * | 2018-12-11 | 2022-01-20 | Kyoto University | Method for inducing deletion in genomic dna |
EP3915636A4 (en) | 2019-01-30 | 2022-03-09 | Nissan Chemical Corporation | HYDRAZIDE COMPOUND AND KINASE INHIBITOR |
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 |
CN114786778A (zh) * | 2019-11-27 | 2022-07-22 | 基因泰克公司 | 治疗性化合物 |
JP7678595B2 (ja) | 2020-02-05 | 2025-05-16 | ザ ロックフェラー ユニバーシティー | ピロロ[2,3‐b]ピリジン‐3‐カルボキサミド組成物及び聴力損失を改善するための方法 |
WO2021178779A1 (en) | 2020-03-06 | 2021-09-10 | Incyte Corporation | 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 |
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 |
MX2022013518A (es) * | 2020-04-28 | 2023-02-01 | 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 |
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 |
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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 |
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CA2682339A1 (en) | 2007-04-06 | 2008-10-16 | Novartis Ag | 2 , 6-naphthyridine derivatives as protein kinase modulators |
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2017
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- 2018-04-26 CN CN202210409194.5A patent/CN114703144A/zh not_active Withdrawn
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