JP2016514100A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016514100A5 JP2016514100A5 JP2015559015A JP2015559015A JP2016514100A5 JP 2016514100 A5 JP2016514100 A5 JP 2016514100A5 JP 2015559015 A JP2015559015 A JP 2015559015A JP 2015559015 A JP2015559015 A JP 2015559015A JP 2016514100 A5 JP2016514100 A5 JP 2016514100A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- unsubstituted
- haloalkyl
- independently
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 249
- 150000001875 compounds Chemical class 0.000 claims description 181
- 150000004820 halides Chemical class 0.000 claims description 124
- 229910052799 carbon Inorganic materials 0.000 claims description 80
- 150000003839 salts Chemical class 0.000 claims description 78
- 125000001424 substituent group Chemical group 0.000 claims description 69
- 229910052757 nitrogen Inorganic materials 0.000 claims description 63
- 229910052739 hydrogen Inorganic materials 0.000 claims description 56
- 125000004432 carbon atom Chemical group C* 0.000 claims description 40
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims description 40
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 29
- 125000001188 haloalkyl group Chemical group 0.000 claims description 29
- 229910052760 oxygen Inorganic materials 0.000 claims description 27
- 229910052717 sulfur Inorganic materials 0.000 claims description 27
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 17
- 208000035475 disorder Diseases 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 230000007547 defect Effects 0.000 claims description 8
- 230000004770 neurodegeneration Effects 0.000 claims description 6
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 6
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 5
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 5
- 208000010392 Bone Fractures Diseases 0.000 claims description 4
- 208000020084 Bone disease Diseases 0.000 claims description 4
- 206010064147 Gastrointestinal inflammation Diseases 0.000 claims description 4
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims description 4
- 208000001132 Osteoporosis Diseases 0.000 claims description 4
- 102000013814 Wnt Human genes 0.000 claims description 4
- 108050003627 Wnt Proteins 0.000 claims description 4
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 4
- 210000000988 bone and bone Anatomy 0.000 claims description 4
- 230000024245 cell differentiation Effects 0.000 claims description 4
- 208000030533 eye disease Diseases 0.000 claims description 4
- 208000018925 gastrointestinal mucositis Diseases 0.000 claims description 4
- 201000008482 osteoarthritis Diseases 0.000 claims description 4
- 206010033103 otosclerosis Diseases 0.000 claims description 4
- 208000028169 periodontal disease Diseases 0.000 claims description 4
- 210000000130 stem cell Anatomy 0.000 claims description 4
- 208000003265 stomatitis Diseases 0.000 claims description 4
- 230000029663 wound healing Effects 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 208000017442 Retinal disease Diseases 0.000 claims description 3
- 206010038923 Retinopathy Diseases 0.000 claims description 3
- 230000004663 cell proliferation Effects 0.000 claims description 3
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims description 3
- 208000002780 macular degeneration Diseases 0.000 claims description 3
- 201000004384 Alopecia Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 208000014644 Brain disease Diseases 0.000 claims description 2
- 206010007747 Cataract congenital Diseases 0.000 claims description 2
- 206010018325 Congenital glaucomas Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 206010012565 Developmental glaucoma Diseases 0.000 claims description 2
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims description 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000007737 Retinal degeneration Diseases 0.000 claims description 2
- 206010038848 Retinal detachment Diseases 0.000 claims description 2
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 230000005856 abnormality Effects 0.000 claims description 2
- 201000011190 diabetic macular edema Diseases 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 208000024963 hair loss Diseases 0.000 claims description 2
- 230000003676 hair loss Effects 0.000 claims description 2
- 230000011132 hemopoiesis Effects 0.000 claims description 2
- 230000000302 ischemic effect Effects 0.000 claims description 2
- 208000037805 labour Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- 230000004258 retinal degeneration Effects 0.000 claims description 2
- 230000004264 retinal detachment Effects 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 230000017423 tissue regeneration Effects 0.000 claims description 2
- 208000022873 Ocular disease Diseases 0.000 claims 2
- 208000008069 Geographic Atrophy Diseases 0.000 claims 1
- 208000007014 Retinitis pigmentosa Diseases 0.000 claims 1
- 206010058990 Venous occlusion Diseases 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 230000009547 development abnormality Effects 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 0 Cc1ccc(*)cc1 Chemical compound Cc1ccc(*)cc1 0.000 description 19
- 238000000034 method Methods 0.000 description 12
- 125000005842 heteroatom Chemical group 0.000 description 5
- 125000001072 heteroaryl group Chemical group 0.000 description 4
- 206010017076 Fracture Diseases 0.000 description 2
- 101000781981 Homo sapiens Protein Wnt-11 Proteins 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 102100036567 Protein Wnt-11 Human genes 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 description 2
- 206010003694 Atrophy Diseases 0.000 description 1
- UAEPNZWRGJTJPN-UHFFFAOYSA-N CC1CCCCC1 Chemical compound CC1CCCCC1 UAEPNZWRGJTJPN-UHFFFAOYSA-N 0.000 description 1
- IEMVYIPRFWIPAS-UHFFFAOYSA-N CN(C)Cc(cccc1)c1C(CCC(c1ncccn1)=O)=O Chemical compound CN(C)Cc(cccc1)c1C(CCC(c1ncccn1)=O)=O IEMVYIPRFWIPAS-UHFFFAOYSA-N 0.000 description 1
- FKNQCJSGGFJEIZ-UHFFFAOYSA-N Cc1ccncc1 Chemical compound Cc1ccncc1 FKNQCJSGGFJEIZ-UHFFFAOYSA-N 0.000 description 1
- 101100317380 Danio rerio wnt4a gene Proteins 0.000 description 1
- 101000814371 Homo sapiens Protein Wnt-10a Proteins 0.000 description 1
- 101000770799 Homo sapiens Protein Wnt-10b Proteins 0.000 description 1
- 101000804728 Homo sapiens Protein Wnt-2b Proteins 0.000 description 1
- 101000804792 Homo sapiens Protein Wnt-5a Proteins 0.000 description 1
- 101000804804 Homo sapiens Protein Wnt-5b Proteins 0.000 description 1
- 101000855002 Homo sapiens Protein Wnt-6 Proteins 0.000 description 1
- 101000855004 Homo sapiens Protein Wnt-7a Proteins 0.000 description 1
- 101000814380 Homo sapiens Protein Wnt-7b Proteins 0.000 description 1
- 101000814350 Homo sapiens Protein Wnt-8a Proteins 0.000 description 1
- 101000650149 Homo sapiens Protein Wnt-8b Proteins 0.000 description 1
- 101000650117 Homo sapiens Protein Wnt-9a Proteins 0.000 description 1
- 101000650119 Homo sapiens Protein Wnt-9b Proteins 0.000 description 1
- 101000781955 Homo sapiens Proto-oncogene Wnt-1 Proteins 0.000 description 1
- 101000954762 Homo sapiens Proto-oncogene Wnt-3 Proteins 0.000 description 1
- NISGSNTVMOOSJQ-UHFFFAOYSA-N NC1CCCC1 Chemical compound NC1CCCC1 NISGSNTVMOOSJQ-UHFFFAOYSA-N 0.000 description 1
- XEBZMOYBOFZHIC-UHFFFAOYSA-N O=C(CCC(c1ncccn1)=O)c1ccc[o]1 Chemical compound O=C(CCC(c1ncccn1)=O)c1ccc[o]1 XEBZMOYBOFZHIC-UHFFFAOYSA-N 0.000 description 1
- SLXIBNFBKHDXNQ-UHFFFAOYSA-N O=C(CCC(c1ncccn1)=O)c1ccccc1 Chemical compound O=C(CCC(c1ncccn1)=O)c1ccccc1 SLXIBNFBKHDXNQ-UHFFFAOYSA-N 0.000 description 1
- IWFBEEVFOIACTB-UHFFFAOYSA-N OCc(cccc1)c1C(CCC(c1ncccn1)=O)=O Chemical compound OCc(cccc1)c1C(CCC(c1ncccn1)=O)=O IWFBEEVFOIACTB-UHFFFAOYSA-N 0.000 description 1
- 102100039461 Protein Wnt-10a Human genes 0.000 description 1
- 102100029062 Protein Wnt-10b Human genes 0.000 description 1
- 102100035289 Protein Wnt-2b Human genes 0.000 description 1
- 102100035331 Protein Wnt-5b Human genes 0.000 description 1
- 102100020732 Protein Wnt-6 Human genes 0.000 description 1
- 102100020729 Protein Wnt-7a Human genes 0.000 description 1
- 102100039470 Protein Wnt-7b Human genes 0.000 description 1
- 102100039453 Protein Wnt-8a Human genes 0.000 description 1
- 102100027542 Protein Wnt-8b Human genes 0.000 description 1
- 102100027503 Protein Wnt-9a Human genes 0.000 description 1
- 102100027502 Protein Wnt-9b Human genes 0.000 description 1
- 101150010310 WNT-4 gene Proteins 0.000 description 1
- 101150019524 WNT2 gene Proteins 0.000 description 1
- 208000000208 Wet Macular Degeneration Diseases 0.000 description 1
- 102000052547 Wnt-1 Human genes 0.000 description 1
- 102000052556 Wnt-2 Human genes 0.000 description 1
- 108700020986 Wnt-2 Proteins 0.000 description 1
- 102000052549 Wnt-3 Human genes 0.000 description 1
- 102000052548 Wnt-4 Human genes 0.000 description 1
- 108700020984 Wnt-4 Proteins 0.000 description 1
- 102000043366 Wnt-5a Human genes 0.000 description 1
- 102000044880 Wnt3A Human genes 0.000 description 1
- 108700013515 Wnt3A Proteins 0.000 description 1
- 101100485099 Xenopus laevis wnt2b-b gene Proteins 0.000 description 1
- 230000037444 atrophy Effects 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000000174 oncolytic effect Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 208000004644 retinal vein occlusion Diseases 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 101150068520 wnt3a gene Proteins 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361768033P | 2013-02-22 | 2013-02-22 | |
| US61/768,033 | 2013-02-22 | ||
| PCT/US2014/017794 WO2014130869A1 (en) | 2013-02-22 | 2014-02-21 | Gamma-diketones as wnt/beta -catenin signaling pathway activators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018166538A Division JP2019031496A (ja) | 2013-02-22 | 2018-09-06 | Ｗｎｔ／β−カテニンシグナル伝達経路活性化剤としてのγ−ジケトン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016514100A JP2016514100A (ja) | 2016-05-19 |
| JP2016514100A5 true JP2016514100A5 (enExample) | 2017-03-23 |
| JP6401189B2 JP6401189B2 (ja) | 2018-10-03 |
Family
ID=51388762
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015559015A Active JP6401189B2 (ja) | 2013-02-22 | 2014-02-21 | Ｗｎｔ／β−カテニンシグナル伝達経路活性化剤としてのγ−ジケトン |
| JP2018166538A Pending JP2019031496A (ja) | 2013-02-22 | 2018-09-06 | Ｗｎｔ／β−カテニンシグナル伝達経路活性化剤としてのγ−ジケトン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018166538A Pending JP2019031496A (ja) | 2013-02-22 | 2018-09-06 | Ｗｎｔ／β−カテニンシグナル伝達経路活性化剤としてのγ−ジケトン |
Country Status (32)
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2464232B1 (en) | 2009-08-10 | 2015-10-07 | Samumed, LLC | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| ES2879314T3 (es) | 2010-08-18 | 2021-11-22 | Biosplice Therapeutics Inc | Dicetonas e hidroxicetonas como activadores de la vía de señalización de catenina |
| PL2968249T3 (pl) | 2013-02-22 | 2019-06-28 | Samumed, Llc | Gamma-diketony jako aktywatory szlaku sygnałowego Wnt/beta-kateniny |
| US9795550B2 (en) | 2014-08-20 | 2017-10-24 | Samumed, Llc | Gamma-diketones for treatment and prevention of aging skin and wrinkles |
| CN104311544A (zh) * | 2014-09-22 | 2015-01-28 | 湖南华腾制药有限公司 | 一种苯并恶唑衍生物的制备方法 |
| CN104292179A (zh) * | 2014-10-19 | 2015-01-21 | 湖南华腾制药有限公司 | 一种2-氯苯并[d]恶唑-5-甲醛的制备方法 |
| BR112017027227B1 (pt) | 2015-06-16 | 2023-12-12 | Eisai R&D Management Co., Ltd | Agente anti-câncer |
| MX2017015257A (es) | 2015-06-23 | 2018-02-19 | Eisai R&D Man Co Ltd | Cristal de (6s, 9as)-n-bencil-8-({6-[3-(4-etilpiperazin-1-il)azeti din-1-il]piridin-2-il}metil)-6-(2-(fluoruro-4-hidroxibencil)-4,7- dioxo-2-prop-2-en-1-il)hexahidro-2h-pirazino[2,1-c] [1,2,4]triazon-1-(6h)-carboxamida. |
| US12303505B2 (en) | 2017-02-08 | 2025-05-20 | Eisai R&D Management Co., Ltd. | Tumor-treating pharmaceutical composition |
| BR112019023064A2 (pt) | 2017-05-16 | 2020-06-09 | Eisai R&D Man Co Ltd | tratamento de carcinoma hepatocelular |
| CN109678687B (zh) * | 2018-12-11 | 2022-02-11 | 沾化大荣化工科技有限公司 | 一种邻羟基苯乙酮类化合物的高效制备方法 |
| CA3136920A1 (en) * | 2019-06-06 | 2020-12-10 | Fermenta Biotech Limited | An improved process to synthesize 5-(3-pyridyl)-2,2'-bithiophene(sensitizer) |
| CN111632147A (zh) * | 2020-06-07 | 2020-09-08 | 重庆医科大学 | 骨细胞Wnt激活剂在制备骨折加速愈合、防治骨不连及不运动或失重骨丢失药物中的应用 |
| EP4173675A1 (en) * | 2021-10-26 | 2023-05-03 | Perha Pharmaceuticals | Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4 |
| CN116808027B (zh) * | 2023-05-30 | 2025-08-29 | 重庆医科大学附属第一医院 | 化合物或其盐在制备抑制wnt7a基因活性的制剂中的应用 |
Family Cites Families (125)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3040054A (en) | 1960-08-03 | 1962-06-19 | Olin Mathieson | 2, 2'-(1, 4-diaminotetramethylene) bis(4-thiazolecarboxylic acid), salts and process |
| US3855675A (en) | 1971-05-25 | 1974-12-24 | Squibb & Sons Inc | 1-(2-furanylmethyl)-1h-pyrazolo(3,4-b)pyridine-5-methanones |
| US4014889A (en) | 1972-12-20 | 1977-03-29 | Bayer Aktiengesellschaft | Process for preparing ketones |
| US4032526A (en) | 1975-10-02 | 1977-06-28 | American Cyanamid Company | 1,2-dimethyl-3 or 5-piperazinyl-pyrazolium salts |
| US4164559A (en) | 1977-09-21 | 1979-08-14 | Cornell Research Foundation, Inc. | Collagen drug delivery device |
| DE2808070A1 (de) | 1978-02-24 | 1979-08-30 | Bayer Ag | Verfahren zur herstellung von 4-pyridon-3-carbonsaeuren und/oder deren derivaten |
| US4761471A (en) | 1980-08-04 | 1988-08-02 | The Regents Of The University Of California | Bone morphogenetic protein composition |
| US4474752A (en) | 1983-05-16 | 1984-10-02 | Merck & Co., Inc. | Drug delivery system utilizing thermosetting gels |
| DE3331692A1 (de) | 1983-09-02 | 1985-03-28 | Basf Ag, 6700 Ludwigshafen | 3-phenyl-4-methoxycarbonylpyrazole, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung unerwuenschten pflanzenwuchses |
| EP0230110A1 (en) | 1985-11-30 | 1987-07-29 | FISONS plc | Pharmacologically active pyrrole and pyrazole derivatives |
| US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
| EP0290442A4 (en) | 1986-11-19 | 1990-07-03 | Chemex Pharmaceuticals Inc | MEDICINAL PREPARATIONS AND MIXTURES THEREOF, ORGANIC COMPOSITIONS AND METAL SALTS. |
| FR2613360B1 (fr) | 1987-04-03 | 1989-06-09 | Oreal | Nouveaux derives aromatiques d'acide butyrique, leur procede de preparation et leur utilisation en medecine humaine et veterinaire ainsi qu'en cosmetique |
| NZ227287A (en) | 1987-12-21 | 1992-01-29 | Merck & Co Inc | 2,5-diaryl tetrahydrofurans and medicaments |
| AU626881B2 (en) | 1988-07-14 | 1992-08-13 | F. Hoffmann-La Roche Ag | Benzofused heterocyclics used as pharmaceuticals |
| IL91418A (en) | 1988-09-01 | 1997-11-20 | Rhone Poulenc Agrochimie | (hetero) cyclic amide derivatives, process for their preparation and fungicidal compositions containing them |
| EP0365089A3 (en) | 1988-10-18 | 1991-06-05 | Merck & Co. Inc. | 2-aryl-5(3-methoxy-5-(hydroxypropylsulfonyl)-4-propoxyphenyl) tetrahydrothiophen and analogs |
| ES2113857T3 (es) | 1989-03-28 | 1998-05-16 | Genetics Inst | Composiciones osteoinductoras. |
| EP0454204B1 (en) | 1990-04-27 | 1995-06-28 | Duphar International Research B.V | Method for the photochemical isomeration of organic compounds under the influence of a photosensitizer |
| DE4104931A1 (de) | 1991-02-18 | 1992-08-20 | Hoechst Ag | Verfahren zur herstellung substituierter indene |
| JPH05170764A (ja) | 1991-12-24 | 1993-07-09 | Sumitomo Pharmaceut Co Ltd | 新規なヒドロキシカルコン誘導体 |
| GB9203806D0 (en) | 1992-02-21 | 1992-04-08 | Unilever Plc | Sunscreen agents |
| DK57892D0 (da) | 1992-05-01 | 1992-05-01 | Nkt Res Center As | Fremgangsmaade til fremstilling af 1,4-bis-aryl-butan-1,4-dioner og poly(arylen-butan-1,4-dioner) |
| DE69520876T2 (de) | 1994-10-07 | 2002-02-21 | Meiji Seika K.K., Tokio/Tokyo | Gamma-diketonverbindung mit thrombozytenaggregationshemmender wirkung |
| AU1726695A (en) | 1995-01-13 | 1996-07-31 | Board Of Regents, The University Of Texas System | Turcasarins, novel expanded porphyrins, and uses thereof |
| US5668148A (en) | 1995-04-20 | 1997-09-16 | Merck & Co., Inc. | Alpha1a adrenergic receptor antagonists |
| US5585118A (en) | 1995-06-02 | 1996-12-17 | Brigham And Women's Hospital | Choline in the treatment of bipolar disorder |
| US5668165A (en) | 1995-06-07 | 1997-09-16 | Scriptgen Pharmaceuticals, Inc. | Small molecule inhibition of RNA/ligand binding |
| JP3964478B2 (ja) | 1995-06-30 | 2007-08-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬 |
| BR9707588A (pt) | 1996-02-19 | 1999-07-27 | Japan Tobacco Inc | Agente terapeutico para diabetes |
| WO1997046225A1 (en) | 1996-06-03 | 1997-12-11 | Purdue Research Foundation | Selenophene anti-tumor agents |
| US6620804B2 (en) | 1996-06-03 | 2003-09-16 | Purdue Research Foundation | Selenophene anti-tumor agents |
| US6440102B1 (en) | 1998-07-23 | 2002-08-27 | Durect Corporation | Fluid transfer and diagnostic system for treating the inner ear |
| WO2000009500A2 (en) | 1998-08-11 | 2000-02-24 | Nihon Bayer Agrochem K.K. | Nematicidal pyrazoles |
| JP2002528533A (ja) | 1998-10-29 | 2002-09-03 | ブリストル−マイヤーズ スクイブ カンパニー | 酵素ｉｍｐｄｈの新規なインヒビター |
| DE19853299C2 (de) | 1998-11-19 | 2003-04-03 | Thomas Lenarz | Katheter zur Applikation von Medikamenten in Flüssigkeitsräumen des menschlichen Innenohrs |
| US6120484A (en) | 1999-02-17 | 2000-09-19 | Silverstein; Herbert | Otological implant for delivery of medicament and method of using same |
| JP2003503386A (ja) | 1999-06-25 | 2003-01-28 | メルク エンド カムパニー インコーポレーテッド | １−（芳香族またはヘテロ芳香族置換）−３−（ヘテロ芳香族置換）−１，３−プロパンジオン類およびそれの使用 |
| EP1067195B1 (de) | 1999-07-09 | 2006-09-20 | Forschungszentrum Jülich Gmbh | Verfahren zur Reduktion von Ketogruppen enthaltende Verbindungen |
| PL211797B1 (pl) | 1999-07-13 | 2012-06-29 | Lonza Ag | Sposób wytwarzania 2-amino-4-(4-fluorofenylo)-6-alkilopirymidyno-5-karboksylanu oraz nowe związki pośrednie i sposoby ich wytwarzania |
| DE60019505T2 (de) | 1999-08-06 | 2005-09-15 | Ciba Speciality Chemicals Holding Inc. | Mikrobizide Wirksubstanzen |
| AUPQ288499A0 (en) | 1999-09-16 | 1999-10-07 | Biota Scientific Management Pty Ltd | Antiviral agents |
| WO2001027116A2 (en) | 1999-10-07 | 2001-04-19 | Eli Lilly And Company | Condensed dihydroquinolinone derivatives for inhibiting mrp1 |
| US6268375B1 (en) | 1999-12-29 | 2001-07-31 | Research Triangle Institute | 10, 11-difluoromethylenedioxycamptothecin compounds with topoisomerase I inhibition |
| US6967023B1 (en) | 2000-01-10 | 2005-11-22 | Foamix, Ltd. | Pharmaceutical and cosmetic carrier or composition for topical application |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| JP2001294581A (ja) | 2000-04-12 | 2001-10-23 | Nippon Bayer Agrochem Co Ltd | イソチアゾール誘導体 |
| US6794362B1 (en) | 2000-05-30 | 2004-09-21 | Connective Tissue Imagineering Llc | Asparagine containing elastin peptide analogs |
| AU7102201A (en) | 2000-07-05 | 2002-01-14 | Yamanouchi Pharma Co Ltd | Propane-1,3-dione derivatives |
| DE10059749A1 (de) | 2000-12-01 | 2002-06-20 | Henkel Kgaa | Fixierung von Wirkstoffen an fasrigen Materialien |
| JP4365094B2 (ja) | 2001-03-02 | 2009-11-18 | メルク フロスト カナダ リミテツド | カテプシンシステインプロテアーゼ阻害薬 |
| ES2292753T4 (es) | 2001-03-29 | 2009-02-16 | Vertex Pharmaceuticals Incorporated | Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas. |
| KR100785109B1 (ko) | 2001-04-05 | 2007-12-12 | 토렌트 파마슈티칼스 리미티드 | 노화 관련 및 당뇨병 혈관성 합병증에 사용되는 헤테로사이클릭 화합물 |
| CA2444882A1 (en) | 2001-04-30 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of gsk-3 and crystal structures of gsk-3.beta. protein and protein complexes |
| US6987123B2 (en) | 2001-07-26 | 2006-01-17 | Cadila Healthcare Limited | Heterocyclic compounds, their preparation, pharmaceutical compositions containing them and their use in medicine |
| WO2003016266A1 (fr) | 2001-08-16 | 2003-02-27 | Japan Tobacco Inc. | Composes $g(b)-cetoamides et leur utilisation medicinale |
| US6648873B2 (en) | 2001-09-21 | 2003-11-18 | Durect Corp. | Aural catheter system including anchor balloon and balloon inflation device |
| KR20050035142A (ko) | 2001-10-11 | 2005-04-15 | 카네카 코포레이션 | 페록시좀 증식제 응답성 수용체 리간드제 및 그 제조 방법 |
| EP1463715A1 (en) * | 2001-12-03 | 2004-10-06 | Novo Nordisk A/S | Novel glucagon antagonists |
| CN1155590C (zh) | 2002-04-12 | 2004-06-30 | 中国药科大学 | 具有抗肿瘤活性的色酮类化合物及其开环产物与制备方法 |
| AU2003265395A1 (en) | 2002-08-14 | 2004-03-03 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| US20040266732A1 (en) | 2002-09-20 | 2004-12-30 | Jorge Galvez | Therapeutic agents, methods, and treatments |
| FR2849598B1 (fr) | 2003-01-07 | 2006-09-22 | Merck Sante Sas | Utilisation d'inhibiteurs de la kynurenine-3-hydroxylase pour le traitement du diabete, par augmentation du nombre de cellules des ilots de langerhans |
| US20040224003A1 (en) | 2003-02-07 | 2004-11-11 | Schultz Robert K. | Drug formulations for coating medical devices |
| ATE387435T1 (de) | 2003-04-15 | 2008-03-15 | Astrazeneca Ab | Substituirte benzosulfonamide als potenzierungsmittel von glutamatrezeptoren |
| KR101415503B1 (ko) | 2003-07-17 | 2014-07-04 | 플렉시콘, 인코퍼레이티드 | Ｐｐａｒ 활성 화합물 |
| US7008953B2 (en) | 2003-07-30 | 2006-03-07 | Agouron Pharmaceuticals, Inc. | 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| US8841326B2 (en) | 2004-02-12 | 2014-09-23 | Stc.Unm | Therapeutic curcumin derivatives |
| US20060276536A1 (en) | 2004-02-12 | 2006-12-07 | Vander Jagt David L | Cancer treatment using curcumin derivatives |
| JP2007526324A (ja) | 2004-03-02 | 2007-09-13 | スミスクライン・ビーチャム・コーポレイション | Ａｋｔ活性のある阻害剤 |
| UA85711C2 (ru) | 2004-05-06 | 2009-02-25 | Зе Регентс Оф Зе Юниверсити Оф Калифорния | Замещенные енаминоны, их производные и их применение |
| EP1752452A4 (en) | 2004-06-04 | 2010-07-14 | Astellas Pharma Inc | DERIVATIVE OF PROPANE-1, 3-DIONE OR ITS SALT |
| DE102004029309A1 (de) | 2004-06-17 | 2005-12-29 | Bayer Cropscience Gmbh | Pyridinylisoxazole und ihre Verwendung als Herbizide |
| EP2298292A3 (en) | 2004-06-18 | 2011-08-10 | Agennix USA Inc. | Kinase inhibitors for treating cancers |
| CA2577169A1 (en) | 2004-08-16 | 2006-02-23 | The University Of Queensland | Metabolism-modulating agents and uses therefor |
| US7351745B2 (en) | 2004-12-22 | 2008-04-01 | Avon Products, Inc | Compositions and methods of their use for improving the condition and appearance of skin |
| FR2880802B1 (fr) | 2005-01-14 | 2008-12-19 | Sederma Soc Par Actions Simpli | Composition cosmetique ou dermopharmaceutique contenant un extrait d'euglene |
| JP2008094720A (ja) | 2005-01-20 | 2008-04-24 | Astellas Pharma Inc | キノロン誘導体のプロドラッグ又はその塩 |
| WO2006079055A2 (en) | 2005-01-24 | 2006-07-27 | Neurosystec Corporation | Apparatus and method for delivering therapeutic and/or other agents to the inner ear and to other tissues |
| MX2007009313A (es) | 2005-02-01 | 2007-09-12 | Wyeth Corp | Amino-piridinas como inhibidores de ????-secretasa. |
| RU2404973C2 (ru) | 2005-03-31 | 2010-11-27 | Астеллас Фарма Инк. | Производное соединение пропан-1,3-диона или его соль |
| US8178727B2 (en) | 2005-06-27 | 2012-05-15 | National University Corporation Tohoku University | Bis(arylmethylidene)acetone compound, anti-cancer agent, carcinogenesis-preventive agent, inhibitor of expression of Ki-Ras, ErbB2, c-Myc and Cycline D1, β-catenin-degrading agent, and p53 expression enhancer |
| DE102005031580A1 (de) | 2005-07-06 | 2007-01-11 | Aicuris Gmbh & Co. Kg | Substituierte Sulfolanylpyrazole und ihre Verwendung |
| JP5368792B2 (ja) | 2005-07-29 | 2013-12-18 | レスバーロジックス コーポレイション | 複合疾患の予防および処置のための薬学的組成物および挿入可能な医療用デバイスによるその送達 |
| WO2007051314A1 (en) | 2005-11-07 | 2007-05-10 | American Diagnostica Inc. | Curcuminoid compounds for inhibiting plasminogen activator inhibitor-1 |
| DE602006018057D1 (de) | 2005-11-10 | 2010-12-16 | Chemocentryx Inc | Substituierte chinolone und verwendungsverfahren |
| WO2007103584A2 (en) | 2006-03-09 | 2007-09-13 | Nanovir, Llc | Polyamides for treating human papilloma virus |
| MX2008013194A (es) | 2006-04-11 | 2008-12-01 | Vertex Pharma | Composiciones utiles como inhibidores de canales de sodio regulados por voltaje. |
| JP2008007428A (ja) | 2006-06-27 | 2008-01-17 | Showa Denko Kk | 皮膚外用シワ防止剤 |
| JPWO2008020625A1 (ja) | 2006-08-17 | 2010-01-07 | 国立大学法人金沢大学 | ジベンゾイルメタン系化合物とそれを有効成分とする医薬組成物 |
| US8088369B2 (en) | 2006-08-30 | 2012-01-03 | Kabushiki Kaisha Yakult Honsha | Anti-wrinkle agent |
| US7875603B2 (en) | 2006-09-21 | 2011-01-25 | Nova Southeastern University | Specific inhibitors for vascular endothelial growth factor receptors |
| JP5207341B2 (ja) | 2006-10-26 | 2013-06-12 | 独立行政法人産業技術総合研究所 | 炎症性サイトカイン産生抑制剤 |
| US7799954B2 (en) * | 2006-11-17 | 2010-09-21 | Abraxis Bioscience, Llc | Dicarbonyl derivatives and methods of use |
| JP5231829B2 (ja) | 2007-02-15 | 2013-07-10 | 石原産業株式会社 | ピリジル−トリアゾロピリミジン誘導体又はその塩、それらを含有する有害生物防除剤並びにそれらの製造方法 |
| WO2008118626A2 (en) | 2007-03-08 | 2008-10-02 | Burnham Institute For Medical Research | Inhibitors of jnk and methods for identifying inhibitors of jnk |
| JP5309318B2 (ja) | 2007-03-09 | 2013-10-09 | 国立大学法人 岡山大学 | エステル、カルボン酸及びアミドの製造方法 |
| WO2008129255A1 (en) | 2007-04-18 | 2008-10-30 | Astrazeneca Ab | 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer |
| KR101404398B1 (ko) | 2007-06-20 | 2014-06-09 | (주)뉴트리 | 주름개선 화장료 조성물 |
| CN101951954A (zh) | 2007-11-02 | 2011-01-19 | 诺瓦提斯公司 | 调节低密度脂蛋白受体相关蛋白6(lrp6)的分子和方法 |
| CN101854924A (zh) | 2007-11-05 | 2010-10-06 | 诺瓦提斯公司 | 测量wnt活化以及治疗wnt相关癌症的方法和组合物 |
| EP2240276B1 (en) | 2007-12-06 | 2020-12-02 | Centre National de la Recherche Scientifique (CNRS) | Iron and copper catalytic systems for cross-coupling reactions |
| JP2009179619A (ja) | 2008-02-01 | 2009-08-13 | Toyo Ink Mfg Co Ltd | 新規オキシムエステル化合物およびそれを含んでなるラジカル重合開始剤および重合性組成物 |
| AU2009219359A1 (en) | 2008-02-27 | 2009-09-03 | Msd Consumer Care, Inc. | Enhanced photostability of suncare compositions containing avobenzone |
| MX2010011258A (es) | 2008-04-14 | 2011-06-20 | Univ Texas | Inhibidores de molecula pequeña del dominio de homologia de pleckstrin y metodos para usar los mismos. |
| EP2271341B1 (en) | 2008-05-08 | 2016-08-17 | Nova Southeastern University | Specific inhibitors for vascular endothelial growth factor receptors |
| AU2009313491A1 (en) | 2008-11-05 | 2011-06-30 | University Of Southern California | Small molecule modulators of epigenetic regulation and their therapeutic applications |
| US20130039998A1 (en) | 2008-12-24 | 2013-02-14 | University Of Washington | Compositions of modulators of the wnt/beta-catenin pathway and benzamide and/or hydroxamic acid derivatives to treat bipolar disorder |
| JP5246715B2 (ja) | 2009-01-27 | 2013-07-24 | 独立行政法人科学技術振興機構 | 蛋白質架橋阻害剤およびその用途 |
| UA103918C2 (en) | 2009-03-02 | 2013-12-10 | Айерем Элелси | N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators |
| WO2011009826A2 (en) | 2009-07-21 | 2011-01-27 | ADAMED Sp.z o.o. | Novel chalcone derivatives with cytotoxic activity |
| ES2879314T3 (es) | 2010-08-18 | 2021-11-22 | Biosplice Therapeutics Inc | Dicetonas e hidroxicetonas como activadores de la vía de señalización de catenina |
| KR101784940B1 (ko) | 2010-08-31 | 2017-10-12 | (주)아모레퍼시픽 | 피부 탄력 개선용 화장료 조성물 |
| US9249087B2 (en) | 2011-02-01 | 2016-02-02 | The Board Of Trustees Of The University Of Illinois | HDAC inhibitors and therapeutic methods using the same |
| KR101285259B1 (ko) | 2011-08-04 | 2013-07-11 | (주)케어젠 | Ｗｎｔ 계열 유래 펩타이드 및 이의 용도 |
| US8871748B2 (en) | 2011-09-07 | 2014-10-28 | Island Kinetics Inc. | Retinal cyclodextrin acetals and hemiacetals for treating skin complexion disorder |
| US9668691B2 (en) | 2011-09-22 | 2017-06-06 | Lvmh Recherche | Method to measure skin elasticity and firmness |
| ES2958619T3 (es) | 2012-01-30 | 2024-02-12 | Univ Gent | Compuestos anti-invasivos |
| US20130302381A1 (en) | 2012-05-09 | 2013-11-14 | Cook Medical Technologies Llc | Implantable Medical Devices Including a Water-Insoluble Therapeutic Agent |
| US8865700B2 (en) | 2012-12-20 | 2014-10-21 | Avon Products, Inc. | Collagen stimulators and their use in the treatment of skin |
| EP3290421B1 (en) | 2013-02-22 | 2019-01-02 | Pfizer Inc | Combination of pyrrolo [2, 3 -d]pyrimidine derivatives with one or more additional agents as inhibitors of janus- related kinases (jak) |
| ME02671B (me) | 2013-02-22 | 2017-06-20 | H Lundbeck As | Postupak za proizvodnju vortioksetina |
| MX2015010682A (es) | 2013-02-22 | 2016-05-31 | Stemcentrx Inc | Nuevos conjugados de anticuerpos y usos de los mismos. |
| PL2968249T3 (pl) | 2013-02-22 | 2019-06-28 | Samumed, Llc | Gamma-diketony jako aktywatory szlaku sygnałowego Wnt/beta-kateniny |
| US9795550B2 (en) | 2014-08-20 | 2017-10-24 | Samumed, Llc | Gamma-diketones for treatment and prevention of aging skin and wrinkles |
-
2014
- 2014-02-21 PL PL14753569T patent/PL2968249T3/pl unknown
- 2014-02-21 SI SI201431058T patent/SI2968249T1/sl unknown
- 2014-02-21 RU RU2015140118A patent/RU2680716C2/ru active
- 2014-02-21 PT PT14753569T patent/PT2968249T/pt unknown
- 2014-02-21 AU AU2014218720A patent/AU2014218720B2/en not_active Ceased
- 2014-02-21 BR BR112015020391-4A patent/BR112015020391B1/pt not_active IP Right Cessation
- 2014-02-21 HR HRP20190142TT patent/HRP20190142T1/hr unknown
- 2014-02-21 SG SG10201606032VA patent/SG10201606032VA/en unknown
- 2014-02-21 CN CN201480022762.XA patent/CN105188696A/zh active Pending
- 2014-02-21 KR KR1020157026034A patent/KR102252567B1/ko active Active
- 2014-02-21 US US14/187,063 patent/US9533976B2/en active Active
- 2014-02-21 ME MEP-2019-28A patent/ME03296B/me unknown
- 2014-02-21 SG SG11201506592SA patent/SG11201506592SA/en unknown
- 2014-02-21 PE PE2015001796A patent/PE20151721A1/es active IP Right Grant
- 2014-02-21 RU RU2019104082A patent/RU2019104082A/ru unknown
- 2014-02-21 DK DK14753569.4T patent/DK2968249T3/en active
- 2014-02-21 JP JP2015559015A patent/JP6401189B2/ja active Active
- 2014-02-21 SM SM20190059T patent/SMT201900059T1/it unknown
- 2014-02-21 EP EP14753569.4A patent/EP2968249B1/en active Active
- 2014-02-21 CA CA2901671A patent/CA2901671C/en active Active
- 2014-02-21 MA MA38421A patent/MA38421A1/fr unknown
- 2014-02-21 MX MX2015010948A patent/MX368663B/es active IP Right Grant
- 2014-02-21 LT LTEP14753569.4T patent/LT2968249T/lt unknown
- 2014-02-21 WO PCT/US2014/017794 patent/WO2014130869A1/en not_active Ceased
- 2014-02-21 MY MYPI2015002083A patent/MY176004A/en unknown
- 2014-02-21 RS RS20190139A patent/RS58432B1/sr unknown
- 2014-02-21 HU HUE14753569A patent/HUE042001T2/hu unknown
- 2014-02-21 ES ES14753569T patent/ES2709824T3/es active Active
- 2014-02-21 EP EP18182474.9A patent/EP3456325A3/en not_active Withdrawn
- 2014-02-21 TR TR2019/01496T patent/TR201901496T4/tr unknown
-
2015
- 2015-08-17 IL IL240628A patent/IL240628B/en active IP Right Grant
- 2015-08-20 PH PH12015501847A patent/PH12015501847A1/en unknown
- 2015-08-21 CL CL2015002363A patent/CL2015002363A1/es unknown
- 2015-09-02 ZA ZA2015/06438A patent/ZA201506438B/en unknown
-
2016
- 2016-06-03 CL CL2016001367A patent/CL2016001367A1/es unknown
- 2016-11-21 US US15/356,903 patent/US9951053B2/en active Active
-
2018
- 2018-03-12 US US15/918,086 patent/US10457672B2/en active Active
- 2018-09-06 JP JP2018166538A patent/JP2019031496A/ja active Pending
- 2018-12-10 AU AU2018275021A patent/AU2018275021A1/en not_active Abandoned
-
2019
- 2019-01-31 CY CY20191100142T patent/CY1122751T1/el unknown
- 2019-09-20 US US16/577,592 patent/US11034682B2/en active Active
-
2021
- 2021-04-27 US US17/241,662 patent/US11673885B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2015140118A (ru) | γ-ДИКЕТОНЫ В КАЧЕСТВЕ АКТИВАТОРОВ WNT/β-КАТЕНИНОВОГО СИГНАЛЬНОГО ПУТИ | |
| RU2016124136A (ru) | Дикетоны и гидроксикетоны в качестве активатора сигнального пути катенина | |
| JP2015515989A5 (enExample) | ||
| RU2014144309A (ru) | Индазольные ингибиторы сигнального пути wnt и их терапевтические применения | |
| JP2015512443A5 (enExample) | ||
| NZ592993A (en) | Compounds for treating ophthalmic diseases and disorders | |
| JP2020506701A5 (enExample) | ||
| IL263314A (en) | Use of agonists of formyl peptide receptor 2 for treating ocular inflammatory diseases | |
| RU2014148773A (ru) | 1н-пиразоло[3,4-b]пиридины и их терапевтические применения | |
| CN109328187A (zh) | 一种具有fgfr抑制活性的新型化合物及其制备和应用 | |
| JP2015503610A5 (enExample) | ||
| JP2016519165A5 (enExample) | ||
| JP2018515495A5 (enExample) | ||
| JP2019535723A5 (enExample) | ||
| RU2016151420A (ru) | Новое терапевтическое применение производных бензилиденгуанидина для лечения протеинопатий | |
| PH12019501251A1 (en) | Novel phenyl propionic acid derivatives and uses thereof | |
| JP2020502092A5 (enExample) | ||
| JP2013522376A5 (enExample) | ||
| JP2016505637A5 (enExample) | ||
| PH12016501651A1 (en) | Triazine compound and use thereof for medical purposes | |
| JP2017524733A5 (enExample) | ||
| CA2727378A1 (en) | New co-crystal compound of rivaroxaban and malonic acid | |
| ATE322895T1 (de) | Coenzym q10 zur behandlung von erkrankungen der augen | |
| DE602008001725D1 (de) | 1-(1-benzylpiperidin-4-yl)benzimidazol-5-carbonsäurederivate zur behandlung von diabetes mellitus | |
| JP2019520344A5 (enExample) |