JP2008543970A5 - - Google Patents
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- JP2008543970A5 JP2008543970A5 JP2008519444A JP2008519444A JP2008543970A5 JP 2008543970 A5 JP2008543970 A5 JP 2008543970A5 JP 2008519444 A JP2008519444 A JP 2008519444A JP 2008519444 A JP2008519444 A JP 2008519444A JP 2008543970 A5 JP2008543970 A5 JP 2008543970A5
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- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- independently
- cor
- con
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 50
- 229910052736 halogen Inorganic materials 0.000 claims 43
- 150000002367 halogens Chemical class 0.000 claims 40
- 125000000217 alkyl group Chemical group 0.000 claims 37
- 125000001188 haloalkyl group Chemical group 0.000 claims 35
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 125000003118 aryl group Chemical group 0.000 claims 23
- 125000004093 cyano group Chemical group *C#N 0.000 claims 20
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 208000035475 disorder Diseases 0.000 claims 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000004104 aryloxy group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000002541 furyl group Chemical group 0.000 claims 5
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 208000002874 Acne Vulgaris Diseases 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 4
- 206010000496 acne Diseases 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 102000006255 nuclear receptors Human genes 0.000 claims 4
- 108020004017 nuclear receptors Proteins 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- -1 C 0 -C 6 alkoxy Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 3
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 230000037365 barrier function of the epidermis Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000001883 cholelithiasis Diseases 0.000 claims 2
- 230000004069 differentiation Effects 0.000 claims 2
- 210000002615 epidermis Anatomy 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 208000006132 lipodystrophy Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 210000004877 mucosa Anatomy 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 210000003491 skin Anatomy 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69437205P | 2005-06-27 | 2005-06-27 | |
| US60/694,372 | 2005-06-27 | ||
| US73612005P | 2005-11-10 | 2005-11-10 | |
| US60/736,120 | 2005-11-10 | ||
| PCT/US2006/024749 WO2007002559A1 (en) | 2005-06-27 | 2006-06-26 | Pyrazole based lxr modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008543970A JP2008543970A (ja) | 2008-12-04 |
| JP2008543970A5 true JP2008543970A5 (https=) | 2010-08-26 |
| JP5237799B2 JP5237799B2 (ja) | 2013-07-17 |
Family
ID=37309323
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008519444A Expired - Fee Related JP5237799B2 (ja) | 2005-06-27 | 2006-06-26 | ピラゾールベースのｌｘｒモジュレーター |
| JP2008519445A Expired - Fee Related JP5244589B2 (ja) | 2005-06-27 | 2006-06-26 | イミダゾールに基づくｌｘｒモジュレーター |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008519445A Expired - Fee Related JP5244589B2 (ja) | 2005-06-27 | 2006-06-26 | イミダゾールに基づくｌｘｒモジュレーター |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US8703805B2 (https=) |
| EP (2) | EP1910307A1 (https=) |
| JP (2) | JP5237799B2 (https=) |
| KR (2) | KR101363278B1 (https=) |
| AR (2) | AR054521A1 (https=) |
| AU (2) | AU2006261841B8 (https=) |
| BR (1) | BRPI0612287A8 (https=) |
| CA (2) | CA2613522A1 (https=) |
| ES (1) | ES2525217T3 (https=) |
| IL (1) | IL188239A0 (https=) |
| MX (1) | MX2008000141A (https=) |
| MY (1) | MY152162A (https=) |
| NO (1) | NO20080391L (https=) |
| NZ (1) | NZ564916A (https=) |
| PE (2) | PE20070187A1 (https=) |
| SG (1) | SG162804A1 (https=) |
| TW (2) | TWI388323B (https=) |
| WO (2) | WO2007002559A1 (https=) |
Families Citing this family (125)
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| PT1558582E (pt) | 2003-07-22 | 2006-05-31 | Arena Pharm Inc | Derivados de diaril- e aril-heteroaril-ureia como moduladores do receptor de serotonina 5-ht2a uteis para a profilaxia e tratamento de desordens relacionadas com o mesmo |
| SA05260357B1 (ar) | 2004-11-19 | 2008-09-08 | ارينا فارماسيتو تيكالز ، أنك | مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به |
| US8703805B2 (en) | 2005-06-27 | 2014-04-22 | Exelixis Patent Company Llc | Modulators of LXR |
| AU2013200480B2 (en) * | 2006-02-28 | 2016-06-09 | Dart Neuroscience (Cayman) Ltd. | Therapeutic compounds |
| EP2562168B1 (en) | 2006-02-28 | 2014-04-16 | Dart Neuroscience (Cayman) Ltd | Therapeutic piperazines as pde4 inhibitors |
| CN101484424B (zh) | 2006-02-28 | 2014-05-14 | 达特神经科学(开曼)有限公司 | 治疗化合物 |
| JP5286254B2 (ja) | 2006-05-18 | 2013-09-11 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ５−ｈｔ２ａセロトニンレセプター活性のモジュレーターとして有用なフェニルピラゾールの結晶形態および調製方法 |
| CA2646076C (en) | 2006-05-18 | 2015-06-30 | Arena Pharmaceuticals, Inc. | Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| ES2536762T3 (es) | 2006-05-18 | 2015-05-28 | Arena Pharmaceuticals, Inc. | Aminas primarias y sus derivados como moduladores del receptor de la serotonina 5-HT2A útiles para el tratamiento de trastornos relacionados con este |
| CA2655933C (en) | 2006-06-23 | 2014-09-09 | Alethia Biotherapeutics Inc. | Polynucleotides and polypeptide sequences involved in cancer |
| TWI408136B (zh) * | 2006-10-02 | 2013-09-11 | Nat Health Research Institutes | 噻吩化合物及其醫藥組成物 |
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| US8193225B2 (en) * | 2006-10-13 | 2012-06-05 | The Board Of Regents Of The University Of Texas System | Isoxazole amides, derivatives and methods of chemical induction of neurogenesis |
| KR20090094125A (ko) * | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Ｌｘｒ 및 ｆｘｒ 조절자 |
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| CN103087043A (zh) * | 2007-03-16 | 2013-05-08 | 中国人民解放军军事医学科学院放射与辐射医学研究所 | 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂 |
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| TWI443090B (zh) | 2007-05-25 | 2014-07-01 | Abbvie Deutschland | 作為代謝性麩胺酸受體２（ｍｇｌｕ２ 受體）之正向調節劑之雜環化合物 |
| US20100197767A1 (en) * | 2007-07-11 | 2010-08-05 | Lior Nissim | Nucleic acid construct systems capable of daignosing or treating a cell state |
| EP2178852B9 (en) | 2007-08-03 | 2016-06-22 | Romark Laboratories, L.C. | Alkylsulfonyl-substituted thiazolide compounds |
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| ITMI20041032A1 (it) * | 2004-05-24 | 2004-08-24 | Neuroscienze S C A R L | Compositi farmaceutici |
| CA2578261A1 (en) | 2004-08-06 | 2006-02-09 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole derivative |
| JP2006104191A (ja) | 2004-09-07 | 2006-04-20 | Sankyo Co Ltd | 置換ビフェニル誘導体 |
| WO2006028029A1 (ja) | 2004-09-07 | 2006-03-16 | Sankyo Company, Limited | 置換ビフェニル誘導体 |
| CA2584317A1 (en) | 2004-10-15 | 2006-04-27 | Memory Pharmaceuticals Corporation | Pyrazole derivatives as phosphodiesterase 4 inhibitors |
| EP2368881A1 (en) | 2005-01-10 | 2011-09-28 | University of Connecticut | Heteropyrazole analogs acting on cannabinoid receptors |
| WO2006076202A1 (en) * | 2005-01-10 | 2006-07-20 | Exelixis, Inc. | Heterocyclic carboxamide compounds as steroid nuclear receptors ligands |
| EP1884513A4 (en) | 2005-05-23 | 2010-04-28 | Japan Tobacco Inc | PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME |
| US8703805B2 (en) | 2005-06-27 | 2014-04-22 | Exelixis Patent Company Llc | Modulators of LXR |
| US20080090834A1 (en) | 2006-07-06 | 2008-04-17 | Pfizer Inc | Selective azole pde10a inhibitor compounds |
| KR20090094125A (ko) | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Ｌｘｒ 및 ｆｘｒ 조절자 |
-
2006
- 2006-06-26 US US11/993,806 patent/US8703805B2/en active Active
- 2006-06-26 KR KR1020087001879A patent/KR101363278B1/ko not_active Expired - Fee Related
- 2006-06-26 JP JP2008519444A patent/JP5237799B2/ja not_active Expired - Fee Related
- 2006-06-26 CA CA002613522A patent/CA2613522A1/en not_active Abandoned
- 2006-06-26 WO PCT/US2006/024749 patent/WO2007002559A1/en not_active Ceased
- 2006-06-26 US US11/993,529 patent/US8569352B2/en not_active Expired - Fee Related
- 2006-06-26 MX MX2008000141A patent/MX2008000141A/es active IP Right Grant
- 2006-06-26 WO PCT/US2006/024757 patent/WO2007002563A1/en not_active Ceased
- 2006-06-26 CA CA002613517A patent/CA2613517A1/en not_active Abandoned
- 2006-06-26 SG SG201004273-7A patent/SG162804A1/en unknown
- 2006-06-26 NZ NZ564916A patent/NZ564916A/en unknown
- 2006-06-26 AU AU2006261841A patent/AU2006261841B8/en not_active Ceased
- 2006-06-26 BR BRPI0612287A patent/BRPI0612287A8/pt not_active IP Right Cessation
- 2006-06-26 AU AU2006261845A patent/AU2006261845C1/en not_active Ceased
- 2006-06-26 EP EP06785558A patent/EP1910307A1/en not_active Withdrawn
- 2006-06-26 ES ES06785562.7T patent/ES2525217T3/es active Active
- 2006-06-26 JP JP2008519445A patent/JP5244589B2/ja not_active Expired - Fee Related
- 2006-06-26 KR KR1020087001957A patent/KR20080028964A/ko not_active Ceased
- 2006-06-26 EP EP06785562.7A patent/EP1910308B1/en active Active
- 2006-06-27 PE PE2006000740A patent/PE20070187A1/es not_active Application Discontinuation
- 2006-06-27 TW TW095123212A patent/TWI388323B/zh not_active IP Right Cessation
- 2006-06-27 MY MYPI20063057 patent/MY152162A/en unknown
- 2006-06-27 AR ARP060102761A patent/AR054521A1/es not_active Application Discontinuation
- 2006-06-27 PE PE2006000741A patent/PE20070105A1/es not_active Application Discontinuation
- 2006-06-27 AR ARP060102762A patent/AR054522A1/es not_active Application Discontinuation
- 2006-06-27 TW TW095123162A patent/TW200745045A/zh unknown
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2007
- 2007-12-19 IL IL188239A patent/IL188239A0/en unknown
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2008
- 2008-01-21 NO NO20080391A patent/NO20080391L/no not_active Application Discontinuation
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2013
- 2013-07-25 US US13/950,772 patent/US9000022B2/en active Active
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