CA2914815A1 - Urea derivatives and uses thereof - Google Patents
Urea derivatives and uses thereof Download PDFInfo
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- CA2914815A1 CA2914815A1 CA2914815A CA2914815A CA2914815A1 CA 2914815 A1 CA2914815 A1 CA 2914815A1 CA 2914815 A CA2914815 A CA 2914815A CA 2914815 A CA2914815 A CA 2914815A CA 2914815 A1 CA2914815 A1 CA 2914815A1
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- substituted
- unsubstituted
- compound
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- 150000003672 ureas Chemical class 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 403
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- 238000000034 method Methods 0.000 claims abstract description 34
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- 208000002780 macular degeneration Diseases 0.000 claims abstract description 20
- 208000027866 inflammatory disease Diseases 0.000 claims abstract description 16
- 208000022873 Ocular disease Diseases 0.000 claims abstract description 15
- 230000011664 signaling Effects 0.000 claims abstract description 14
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- 206010060999 Benign neoplasm Diseases 0.000 claims abstract description 9
- 230000002062 proliferating effect Effects 0.000 claims abstract description 9
- 206010030113 Oedema Diseases 0.000 claims abstract description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 426
- 125000000217 alkyl group Chemical group 0.000 claims description 302
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 289
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 258
- 125000001072 heteroaryl group Chemical group 0.000 claims description 240
- 229910052757 nitrogen Inorganic materials 0.000 claims description 233
- 125000003118 aryl group Chemical group 0.000 claims description 204
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 169
- 229910052717 sulfur Inorganic materials 0.000 claims description 159
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 147
- 125000004429 atom Chemical group 0.000 claims description 147
- 229910052760 oxygen Inorganic materials 0.000 claims description 137
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- 150000003839 salts Chemical class 0.000 claims description 105
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 103
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- 229910052736 halogen Inorganic materials 0.000 claims description 92
- 150000002367 halogens Chemical class 0.000 claims description 92
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 70
- 125000002252 acyl group Chemical group 0.000 claims description 66
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 51
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 49
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- 125000004434 sulfur atom Chemical group 0.000 claims description 33
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 22
- 201000011510 cancer Diseases 0.000 claims description 12
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 11
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 11
- 229910001868 water Inorganic materials 0.000 claims description 11
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 10
- 125000003566 oxetanyl group Chemical group 0.000 claims description 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 8
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- 125000001424 substituent group Chemical group 0.000 description 40
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 39
- 125000001624 naphthyl group Chemical group 0.000 description 39
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- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 34
- 125000000547 substituted alkyl group Chemical group 0.000 description 34
- 239000000463 material Substances 0.000 description 33
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- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 31
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 31
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- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 description 28
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 27
- 125000004076 pyridyl group Chemical group 0.000 description 26
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 26
- 230000033115 angiogenesis Effects 0.000 description 24
- 210000001508 eye Anatomy 0.000 description 24
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- 125000002619 bicyclic group Chemical group 0.000 description 22
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- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 21
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 21
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- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 20
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 19
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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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- Health & Medical Sciences (AREA)
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- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
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| US201361898720P | 2013-11-01 | 2013-11-01 | |
| US61/898,720 | 2013-11-01 | ||
| PCT/US2014/041930 WO2014201127A2 (en) | 2013-06-11 | 2014-06-11 | Urea derivatives and uses thereof |
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| CA2914815A1 (en) | 2013-06-11 | 2014-12-18 | Kala Pharmaceuticals, Inc. | Urea derivatives and uses thereof |
| EP3230272B1 (en) | 2014-12-10 | 2020-08-19 | Kala Pharmaceuticals, Inc. | 1-amino-triazolo(1,5-a)pyridine-substituted urea derivative and uses thereof |
| SG11201804210XA (en) * | 2015-11-20 | 2018-06-28 | Mingsight Pharmaceuticals Inc | Treatment of autoimmune disease |
| WO2018090974A1 (zh) * | 2016-11-17 | 2018-05-24 | 思路迪(北京)医药科技有限公司 | 一种具有抗癌作用的化合物及其制备方法和应用 |
| CN114269339A (zh) | 2019-12-16 | 2022-04-01 | 苏州锐明新药研发有限公司 | 一种萘脲类化合物的应用 |
| CN115348957B (zh) * | 2019-12-31 | 2025-11-25 | 诺华制药股份有限公司 | 用于治疗与sting活性有关的疾病的化合物和组合物 |
| FI4146348T3 (fi) | 2020-05-08 | 2024-09-25 | Halia Therapeutics Inc | Nek7-kinaasin estäjiä |
| CN115487183B (zh) * | 2021-06-18 | 2024-07-26 | 苏州锐明新药研发有限公司 | 萘脲类化合物在制备治疗翼状胬肉的药物中的应用 |
| EP4635495A1 (en) * | 2022-12-13 | 2025-10-22 | Suzhou Raymon Pharmaceuticals Company, Ltd. | Use of naphthylurea compounds in preparation of drugs for treating pterygium |
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| FR2638359A1 (fr) | 1988-11-03 | 1990-05-04 | Tino Dalto | Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau |
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| SE9102652D0 (sv) | 1991-09-13 | 1991-09-13 | Kabi Pharmacia Ab | Injection needle arrangement |
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| EP1683796A1 (en) * | 2005-01-24 | 2006-07-26 | Schering Aktiengesellschaft | Pyrazolopyridines, their preparation and their medical use |
| TW200640443A (en) * | 2005-02-23 | 2006-12-01 | Alcon Inc | Methods for treating ocular angiogenesis, retinal edema, retinal ischemia, and diabetic retinopathy using selective RTK inhibitors |
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| CN101239978A (zh) * | 2008-03-05 | 2008-08-13 | 南方医科大学 | 一种咪唑并吡啶类化合物 |
| WO2011047256A1 (en) * | 2009-10-16 | 2011-04-21 | Duke University | Compositions and methods for the treatment of drug-induced hand-foot syndrome |
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| CA2914815A1 (en) | 2013-06-11 | 2014-12-18 | Kala Pharmaceuticals, Inc. | Urea derivatives and uses thereof |
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2014
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- 2014-06-11 EP EP14811423.4A patent/EP3030239A4/en not_active Withdrawn
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- 2014-06-11 AU AU2014278231A patent/AU2014278231B2/en not_active Ceased
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2015
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2017
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2018
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2019
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2020
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2022
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| AU2020233692B2 (en) | Urea derivatives and uses thereof | |
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| US20210380588A1 (en) | Novel Compounds and Uses Thereof |
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