JP2016530296A5 - - Google Patents
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- Publication number
- JP2016530296A5 JP2016530296A5 JP2016540374A JP2016540374A JP2016530296A5 JP 2016530296 A5 JP2016530296 A5 JP 2016530296A5 JP 2016540374 A JP2016540374 A JP 2016540374A JP 2016540374 A JP2016540374 A JP 2016540374A JP 2016530296 A5 JP2016530296 A5 JP 2016530296A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- acceptable salt
- pharmaceutically acceptable
- aryl
- compound
- 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
- 150000001875 compounds Chemical class 0.000 claims 28
- 150000003839 salts Chemical class 0.000 claims 26
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- -1 -C 1 -C 6 alkyl-aryl Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 206010014476 Elevated cholesterol Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 238000008214 LDL Cholesterol Methods 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000037819 metastatic cancer Diseases 0.000 claims 1
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims 1
- 208000021039 metastatic melanoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361873755P | 2013-09-04 | 2013-09-04 | |
| US61/873,755 | 2013-09-04 | ||
| PCT/US2014/054043 WO2015035015A1 (en) | 2013-09-04 | 2014-09-04 | Liver x receptor (lxr) modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019075449A Division JP6821737B2 (ja) | 2013-09-04 | 2019-04-11 | 肝臓ｘ受容体（ｌｘｒ）のモジュレーター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016530296A JP2016530296A (ja) | 2016-09-29 |
| JP2016530296A5 true JP2016530296A5 (enExample) | 2017-10-12 |
| JP6806961B2 JP6806961B2 (ja) | 2021-01-06 |
Family
ID=52628918
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540374A Expired - Fee Related JP6806961B2 (ja) | 2013-09-04 | 2014-09-04 | 肝臓ｘ受容体（ｌｘｒ）のモジュレーター |
| JP2019075449A Expired - Fee Related JP6821737B2 (ja) | 2013-09-04 | 2019-04-11 | 肝臓ｘ受容体（ｌｘｒ）のモジュレーター |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019075449A Expired - Fee Related JP6821737B2 (ja) | 2013-09-04 | 2019-04-11 | 肝臓ｘ受容体（ｌｘｒ）のモジュレーター |
Country Status (23)
| Country | Link |
|---|---|
| US (7) | US10047055B2 (enExample) |
| EP (2) | EP3041835B1 (enExample) |
| JP (2) | JP6806961B2 (enExample) |
| KR (1) | KR102281803B1 (enExample) |
| CN (2) | CN110003108A (enExample) |
| AU (1) | AU2014315280B2 (enExample) |
| BR (1) | BR112016004904B1 (enExample) |
| CA (1) | CA2923175C (enExample) |
| CY (1) | CY1124057T1 (enExample) |
| DK (1) | DK3041835T3 (enExample) |
| ES (1) | ES2804304T3 (enExample) |
| HR (1) | HRP20201054T1 (enExample) |
| HU (1) | HUE051094T2 (enExample) |
| IL (1) | IL244418B (enExample) |
| LT (1) | LT3041835T (enExample) |
| MX (1) | MX371343B (enExample) |
| PL (1) | PL3041835T3 (enExample) |
| PT (1) | PT3041835T (enExample) |
| RS (1) | RS60479B1 (enExample) |
| SG (1) | SG11201601640SA (enExample) |
| SI (1) | SI3041835T1 (enExample) |
| SM (1) | SMT202000490T1 (enExample) |
| WO (1) | WO2015035015A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3441390A1 (en) | 2012-03-02 | 2019-02-13 | Ralexar Therapeutics, Inc. | Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions |
| SG11201601644RA (en) | 2013-09-04 | 2016-04-28 | Alexar Therapeutics Inc | Liver x receptor (lxr) modulators |
| AU2014315280B2 (en) | 2013-09-04 | 2019-01-24 | Ellora Therapeutics, Inc. | Liver X receptor (LXR) modulators |
| CN110305141B (zh) | 2019-07-18 | 2022-01-11 | 深圳市三启药物开发有限公司 | 一种螺(3,3’-异丙基吡咯烷氧化吲哚)类肝x受体调节剂及其制备方法和应用 |
Family Cites Families (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4353905A (en) * | 1981-09-17 | 1982-10-12 | Warner-Lambert Company | Substituted 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and 6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones |
| US20040072868A1 (en) | 2000-09-18 | 2004-04-15 | Collins Jon Loren | Substitued aminopropoxyaryl derivatives useful as agonists for lxr |
| AUPR738301A0 (en) | 2001-08-30 | 2001-09-20 | Starpharma Limited | Chemotherapeutic agents |
| US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| CA2486651A1 (en) | 2002-05-24 | 2003-12-04 | Pharmacia Corporation | Sulfone liver x-receptor modulators |
| US6900244B2 (en) | 2002-05-24 | 2005-05-31 | Pharmacia Corporation | Anilino liver X-receptor modulators |
| EP1572660B1 (en) | 2002-12-20 | 2011-01-26 | X-Ceptor Therapeutics, Inc. | Isoquinolinone derivatives and their use as therapeutic agents |
| US20060270628A1 (en) | 2003-04-29 | 2006-11-30 | Jagattaran Das | Antiinfective 1,2,3-triazole derivatives, process for their preparation and pharmaceutical compositions containing them |
| EP1628666B1 (en) | 2003-05-14 | 2015-09-23 | NeuroGenetic Pharmaceuticals, Inc. | Compouds and uses thereof in modulating amyloid beta |
| JP2006193426A (ja) | 2003-09-05 | 2006-07-27 | Sankyo Co Ltd | 置換された縮環ピリミジン−４（３ｈ）−オン化合物 |
| US20050245543A1 (en) | 2004-04-30 | 2005-11-03 | Pfizer Inc | Histamine-3 receptor antagonists |
| WO2005113499A1 (ja) | 2004-05-20 | 2005-12-01 | Sankyo Company, Limited | インドール化合物 |
| TW200606133A (en) | 2004-06-30 | 2006-02-16 | Sankyo Co | Substituted benzene compounds |
| AU2005271737A1 (en) | 2004-08-03 | 2006-02-16 | Wyeth | Indazoles useful in treating cardiovascular diseases |
| US20070060589A1 (en) | 2004-12-21 | 2007-03-15 | Purandare Ashok V | Inhibitors of protein arginine methyl transferases |
| WO2006109633A1 (ja) | 2005-04-07 | 2006-10-19 | Daiichi Sankyo Company, Limited | 置換インドール化合物 |
| US7213797B2 (en) | 2005-05-20 | 2007-05-08 | Garland Jerome Gaskins | Deck board straightener |
| CN101248049B (zh) * | 2005-06-27 | 2013-08-28 | 埃克塞利希斯专利有限责任公司 | 咪唑类lxr调节剂 |
| WO2007002563A1 (en) * | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Imidazole based lxr modulators |
| AU2006290442B2 (en) | 2005-09-16 | 2010-07-29 | Arrow Therapeutics Limited | Biphenyl derivatives and their use in treating hepatitis C |
| WO2007034279A2 (en) * | 2005-09-19 | 2007-03-29 | Pfizer Products Inc. | C3a antagonists and pharmaceutical compositions thereof |
| WO2007092065A2 (en) | 2005-11-14 | 2007-08-16 | Irm Llc | Compounds and compositions as lxr modulators |
| EP1849781A1 (en) | 2006-04-28 | 2007-10-31 | Laboratorios del Dr. Esteve S.A. | Substituted 3-Amino-4-hydroxy pyrrolidines compounds, their preparation and use as medicaments |
| TW200825054A (en) | 2006-10-18 | 2008-06-16 | Wyeth Corp | Quinoline compounds |
| WO2008073825A1 (en) | 2006-12-08 | 2008-06-19 | Exelixis, Inc. | Lxr and fxr modulators |
| US8338437B2 (en) | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
| MX2009012474A (es) | 2007-05-18 | 2009-12-18 | Wyeth Corp | Compuestos de quinazolina. |
| US20090069288A1 (en) | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
| CN103772299A (zh) | 2007-08-13 | 2014-05-07 | 霍夫曼-拉罗奇有限公司 | 新型哌嗪酰胺衍生物 |
| BRPI0821315A2 (pt) | 2007-12-21 | 2019-09-24 | Wyeth Llc | compostos benzimidazol |
| BRPI0822237A2 (pt) | 2007-12-21 | 2015-06-30 | Wyeth Llc | Compostos de imidazo [1,2-a] piridina |
| US20120015988A1 (en) | 2008-05-13 | 2012-01-19 | Boehringer Ingelheim International Gmbh | Sulfone Compounds Which Modulate The CB2 Receptor |
| US8063088B2 (en) | 2008-06-11 | 2011-11-22 | Hoffmann-La Roche Inc. | Imidazolidine derivatives |
| JP2012508250A (ja) | 2008-11-07 | 2012-04-05 | ワイス・エルエルシー | キノキサリン系のｌｘｒモジュレーター |
| EP2367801A1 (en) | 2008-11-19 | 2011-09-28 | Wyeth LLC | Polar quinazolines as liver x receptors ( lxrs ) modulators |
| CA2747744A1 (en) * | 2008-12-22 | 2010-07-01 | Theodros Asberom | Gamma secretase modulators |
| US20120058133A1 (en) | 2009-02-19 | 2012-03-08 | President And Fellows Of Harvard College | Inhibition of trna synthetases and therapeutic applications thereof |
| WO2010096777A1 (en) | 2009-02-23 | 2010-08-26 | Presidio Pharmaceuticals, Inc. | Inhibitors of hcv ns5a |
| HRP20170194T1 (hr) | 2009-05-28 | 2017-05-19 | Exelixis Patent Company Llc | Lxr modulatori |
| EP2501696B1 (en) | 2009-10-15 | 2016-12-28 | Guerbet | Imaging agents and their use for the diagnostic in vivo of neurodegenerative diseases, notably alzheimer's disease and derivative diseases |
| GB0919757D0 (en) | 2009-11-12 | 2009-12-30 | Johnson Matthey Plc | Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs |
| WO2012019093A1 (en) | 2010-08-05 | 2012-02-09 | Human Biomolecular Research Institute | Synthetic compounds and methods to decrease nicotine self-administration |
| WO2012020820A1 (ja) | 2010-08-11 | 2012-02-16 | 大正製薬株式会社 | ヘテロアリール－ピラゾール誘導体 |
| CN103180316A (zh) | 2010-08-27 | 2013-06-26 | 钙医学公司 | 调节细胞内钙的化合物 |
| CN102584705B (zh) * | 2011-01-18 | 2015-05-13 | 中国中化股份有限公司 | 3-羟基-取代吡唑的制备方法 |
| AR088728A1 (es) | 2011-03-25 | 2014-07-02 | Bristol Myers Squibb Co | Moduladores de lxr como prodroga de imidazol |
| EP3441390A1 (en) | 2012-03-02 | 2019-02-13 | Ralexar Therapeutics, Inc. | Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions |
| ES2765573T3 (es) | 2012-08-13 | 2020-06-09 | Univ Rockefeller | Tratamiento y diagnóstico de melanoma |
| JP6137184B2 (ja) | 2012-08-27 | 2017-05-31 | コニカミノルタ株式会社 | 有機エレクトロルミネッセンス素子、照明装置及び表示装置 |
| JP5874679B2 (ja) | 2013-04-25 | 2016-03-02 | トヨタ自動車株式会社 | 燃料電池 |
| SG11201601644RA (en) | 2013-09-04 | 2016-04-28 | Alexar Therapeutics Inc | Liver x receptor (lxr) modulators |
| AU2014315280B2 (en) | 2013-09-04 | 2019-01-24 | Ellora Therapeutics, Inc. | Liver X receptor (LXR) modulators |
-
2014
- 2014-09-04 AU AU2014315280A patent/AU2014315280B2/en not_active Ceased
- 2014-09-04 JP JP2016540374A patent/JP6806961B2/ja not_active Expired - Fee Related
- 2014-09-04 SG SG11201601640SA patent/SG11201601640SA/en unknown
- 2014-09-04 US US14/916,275 patent/US10047055B2/en active Active
- 2014-09-04 ES ES14842802T patent/ES2804304T3/es active Active
- 2014-09-04 CA CA2923175A patent/CA2923175C/en not_active Expired - Fee Related
- 2014-09-04 EP EP14842802.2A patent/EP3041835B1/en active Active
- 2014-09-04 WO PCT/US2014/054043 patent/WO2015035015A1/en not_active Ceased
- 2014-09-04 KR KR1020167008708A patent/KR102281803B1/ko not_active Expired - Fee Related
- 2014-09-04 RS RS20200783A patent/RS60479B1/sr unknown
- 2014-09-04 SM SM20200490T patent/SMT202000490T1/it unknown
- 2014-09-04 PL PL14842802T patent/PL3041835T3/pl unknown
- 2014-09-04 HU HUE14842802A patent/HUE051094T2/hu unknown
- 2014-09-04 SI SI201431603T patent/SI3041835T1/sl unknown
- 2014-09-04 CN CN201811528469.7A patent/CN110003108A/zh active Pending
- 2014-09-04 EP EP19194067.5A patent/EP3626712A3/en not_active Withdrawn
- 2014-09-04 HR HRP20201054TT patent/HRP20201054T1/hr unknown
- 2014-09-04 BR BR112016004904-7A patent/BR112016004904B1/pt not_active IP Right Cessation
- 2014-09-04 DK DK14842802.2T patent/DK3041835T3/da active
- 2014-09-04 LT LTEP14842802.2T patent/LT3041835T/lt unknown
- 2014-09-04 MX MX2016002931A patent/MX371343B/es active IP Right Grant
- 2014-09-04 PT PT148428022T patent/PT3041835T/pt unknown
- 2014-09-04 CN CN201480057481.8A patent/CN105658636B/zh not_active Expired - Fee Related
-
2016
- 2016-03-03 IL IL24441816A patent/IL244418B/en active IP Right Grant
-
2018
- 2018-08-03 US US16/054,884 patent/US10246419B2/en active Active
-
2019
- 2019-02-06 US US16/269,444 patent/US11034657B2/en not_active Expired - Fee Related
- 2019-04-11 JP JP2019075449A patent/JP6821737B2/ja not_active Expired - Fee Related
-
2020
- 2020-07-06 CY CY20201100620T patent/CY1124057T1/el unknown
-
2021
- 2021-05-07 US US17/315,035 patent/US20210269406A1/en not_active Abandoned
- 2021-12-15 US US17/552,287 patent/US20220106274A1/en not_active Abandoned
-
2022
- 2022-07-28 US US17/876,354 patent/US20220388963A1/en not_active Abandoned
-
2023
- 2023-03-09 US US18/181,451 patent/US20230212127A1/en not_active Abandoned
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