JP2009514954A5 - - Google Patents
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- JP2009514954A5 JP2009514954A5 JP2008540085A JP2008540085A JP2009514954A5 JP 2009514954 A5 JP2009514954 A5 JP 2009514954A5 JP 2008540085 A JP2008540085 A JP 2008540085A JP 2008540085 A JP2008540085 A JP 2008540085A JP 2009514954 A5 JP2009514954 A5 JP 2009514954A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- compound
- pharmaceutical formulation
- trpv3
- nhso
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 51
- 125000000217 alkyl group Chemical group 0.000 claims 46
- 239000008194 pharmaceutical composition Substances 0.000 claims 34
- 102000003568 TRPV3 Human genes 0.000 claims 29
- 101150043371 Trpv3 gene Proteins 0.000 claims 29
- 125000003545 alkoxy group Chemical group 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 24
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 125000001424 substituent group Chemical group 0.000 claims 17
- 208000002193 Pain Diseases 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000005647 linker group Chemical group 0.000 claims 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 14
- -1 nitro, amino Chemical group 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000004442 acylamino group Chemical group 0.000 claims 9
- 125000004423 acyloxy group Chemical group 0.000 claims 9
- 150000001408 amides Chemical class 0.000 claims 9
- 125000004429 atom Chemical group 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 150000002576 ketones Chemical class 0.000 claims 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims 9
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 230000005764 inhibitory process Effects 0.000 claims 8
- 230000001404 mediated effect Effects 0.000 claims 8
- 230000000903 blocking effect Effects 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 6
- 239000005977 Ethylene Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 150000003568 thioethers Chemical class 0.000 claims 6
- 150000001299 aldehydes Chemical class 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 5
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 5
- 150000001721 carbon Chemical group 0.000 claims 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- 239000002207 metabolite Substances 0.000 claims 5
- 230000001590 oxidative effect Effects 0.000 claims 5
- 239000000651 prodrug Substances 0.000 claims 5
- 229940002612 prodrug Drugs 0.000 claims 5
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical group OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 claims 5
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 101001047090 Homo sapiens Potassium voltage-gated channel subfamily H member 2 Proteins 0.000 claims 4
- 102100022807 Potassium voltage-gated channel subfamily H member 2 Human genes 0.000 claims 4
- 102000003570 TRPV5 Human genes 0.000 claims 4
- 102000003569 TRPV6 Human genes 0.000 claims 4
- 101150096736 TRPV6 gene Proteins 0.000 claims 4
- 101150034091 Trpv5 gene Proteins 0.000 claims 4
- 102000037089 Uniporters Human genes 0.000 claims 4
- 108091006293 Uniporters Proteins 0.000 claims 4
- 150000001540 azides Chemical class 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 4
- 230000002438 mitochondrial effect Effects 0.000 claims 4
- 229940124530 sulfonamide Drugs 0.000 claims 4
- 150000003456 sulfonamides Chemical class 0.000 claims 4
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000003779 hair growth Effects 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 102000003678 AMPA Receptors Human genes 0.000 claims 2
- 108090000078 AMPA Receptors Proteins 0.000 claims 2
- 201000004384 Alopecia Diseases 0.000 claims 2
- 206010058019 Cancer Pain Diseases 0.000 claims 2
- 206010057254 Connective tissue inflammation Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 208000024720 Fabry Disease Diseases 0.000 claims 2
- 206010065390 Inflammatory pain Diseases 0.000 claims 2
- 208000001294 Nociceptive Pain Diseases 0.000 claims 2
- 206010031009 Oral pain Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 102000003566 TRPV1 Human genes 0.000 claims 2
- 101150016206 Trpv1 gene Proteins 0.000 claims 2
- 239000000058 anti acne agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 230000002682 anti-psoriatic effect Effects 0.000 claims 2
- 230000001153 anti-wrinkle effect Effects 0.000 claims 2
- 229940124340 antiacne agent Drugs 0.000 claims 2
- 239000003429 antifungal agent Substances 0.000 claims 2
- 229940121375 antifungal agent Drugs 0.000 claims 2
- 239000004599 antimicrobial Substances 0.000 claims 2
- 239000002282 antimigraine agent Substances 0.000 claims 2
- 229940125684 antimigraine agent Drugs 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003966 growth inhibitor Substances 0.000 claims 2
- 230000003676 hair loss Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 239000003410 keratolytic agent Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 230000004783 oxidative metabolism Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 208000033830 Hot Flashes Diseases 0.000 claims 1
- 206010060800 Hot flush Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010037660 Pyrexia Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000003389 potentiating effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 0 *Oc(cccc1IC(N2c3ccccc3)=Nc3ccccc3C2=O)c1O* Chemical compound *Oc(cccc1IC(N2c3ccccc3)=Nc3ccccc3C2=O)c1O* 0.000 description 2
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73338405P | 2005-11-04 | 2005-11-04 | |
| US79921206P | 2006-05-09 | 2006-05-09 | |
| US83860906P | 2006-08-18 | 2006-08-18 | |
| PCT/US2006/042930 WO2007056124A2 (en) | 2005-11-04 | 2006-11-03 | Compounds for modulating trpv3 function |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009514954A JP2009514954A (ja) | 2009-04-09 |
| JP2009514954A5 true JP2009514954A5 (https=) | 2009-12-24 |
Family
ID=38006999
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008540085A Pending JP2009514954A (ja) | 2005-11-04 | 2006-11-03 | Ｔｒｐｖ３機能を変調するための化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (4) | US7893260B2 (https=) |
| EP (1) | EP1954283A2 (https=) |
| JP (1) | JP2009514954A (https=) |
| CN (1) | CN101355946B (https=) |
| AU (1) | AU2006311883A1 (https=) |
| CA (1) | CA2628441A1 (https=) |
| TW (1) | TWI409070B (https=) |
| WO (1) | WO2007056124A2 (https=) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2392328A1 (en) * | 2005-05-09 | 2011-12-07 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 Function |
| US8916550B2 (en) * | 2005-05-09 | 2014-12-23 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
| EP1948161B1 (en) * | 2005-06-27 | 2012-01-04 | Newtree Co., Ltd. | Method for preventing and treating conditions mediated by ppar using macelignan |
| US7893260B2 (en) * | 2005-11-04 | 2011-02-22 | Hydra Biosciences, Inc. | Substituted quinazolin-4-one compounds for antagonizing TRPV3 function |
| CA2660957C (en) | 2006-08-23 | 2016-10-11 | Neurogen Corporation | 2-phenoxy pyrimidinone analogues |
| US7998980B2 (en) | 2006-09-15 | 2011-08-16 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
| WO2008140750A1 (en) * | 2007-05-10 | 2008-11-20 | Hydra Biosciences Inc. | Compounds for modulating trpv3 function |
| KR100933559B1 (ko) | 2007-10-01 | 2009-12-23 | 재단법인서울대학교산학협력재단 | ３Ｈ-퀴나졸린-４-온 유도체를 함유하는 Ｈｓｐ９０ 억제제및 이를 이용한 항암제 |
| WO2009084034A2 (en) * | 2007-12-18 | 2009-07-09 | Glenmark Pharmaceuticals, S. A. | Chromane derivatives as trpv3 modulators |
| CA2724008A1 (en) * | 2008-01-11 | 2009-09-11 | Glenmark Pharmaceuticals, S.A. | Fused pyrimidine derivatives as trpv3 modulators |
| US8119647B2 (en) * | 2008-04-23 | 2012-02-21 | Glenmark Pharmaceuticals S.A. | Fused pyrimidineone compounds as TRPV3 modulators |
| MX2010011762A (es) * | 2008-06-17 | 2011-02-03 | Glenmark Pharmaceuticals Sa | Derivados de cromano como moduladores del trpv3. |
| WO2010055384A1 (en) * | 2008-11-17 | 2010-05-20 | Glenmark Pharmaceuticals S.A. | Chromenone derivatives as trpv3 antagonists |
| KR101034300B1 (ko) * | 2008-12-02 | 2011-05-16 | 고려대학교 산학협력단 | Ｔｒｐｖ３ 활성 억제 약물 및 이의 활용 |
| KR101034299B1 (ko) * | 2008-12-02 | 2011-05-16 | 고려대학교 산학협력단 | Ｔｒｐｖ３ 활성 조절 약물 및 이의 활용 |
| US8318928B2 (en) * | 2008-12-15 | 2012-11-27 | Glenmark Pharmaceuticals, S.A. | Fused imidazole carboxamides as TRPV3 modulators |
| JP2012514577A (ja) | 2008-12-26 | 2012-06-28 | グレンマーク ファーマシューティカルズ， エセ．アー． | Ｔｒｐｖ３アンタゴニストとしての縮合イミダゾール誘導体 |
| US20110319416A1 (en) * | 2009-01-28 | 2011-12-29 | Emory University | Subunit Selective NMDA Receptor Antagonists For The Treatment Of Neurological Conditions |
| EP2521548A2 (en) * | 2009-11-27 | 2012-11-14 | Proteologics, Ltd | Quinazolin-4(3a)-one derivatives and methods of use thereof |
| MX2013001612A (es) | 2010-08-10 | 2013-07-05 | Abbvie Inc | Moduladores de trpv3 novedosos. |
| US9216177B2 (en) | 2011-02-28 | 2015-12-22 | Drexel University | Small molecular inhibitors of RAD51 recombinase and methods thereof |
| US9012651B2 (en) | 2011-03-24 | 2015-04-21 | Abbvie Inc. | TRPV3 modulators |
| CN102994508B (zh) * | 2011-09-14 | 2015-04-01 | 深圳华大基因科技有限公司 | Olmsted综合征相关基因的鉴别以及与其相关的产品、方法及用途 |
| WO2013062964A2 (en) | 2011-10-24 | 2013-05-02 | Abbvie Inc. | Novel trpv3 modulators |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US9452973B2 (en) | 2012-05-04 | 2016-09-27 | The United States Of America, As Represented By The Secretary Department Of Health And Human Services | Modulators of the relaxin receptor 1 |
| JP2016510749A (ja) * | 2013-03-05 | 2016-04-11 | ユニヴァーシティー オブ ノートル ダム デュ ラック | キナゾリノン抗生物質 |
| PT3052485T (pt) | 2013-10-04 | 2021-10-22 | Infinity Pharmaceuticals Inc | Compostos heterocíclicos e suas utilizações |
| US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| MX382033B (es) | 2014-03-19 | 2025-03-13 | Infinity Pharmaceuticals Inc | Compuestos heterocíclicos para utilizarlos en el tratamiento de trastornos mediados por pi3k-gamma. |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN104744379B (zh) * | 2015-03-13 | 2017-10-27 | 三峡大学 | 一种喹唑啉酮类化合物及其合成方法 |
| WO2016160938A1 (en) | 2015-04-02 | 2016-10-06 | Abbvie Inc. | N-(1,3-thiazol-2-yl)pyrimidine-5-carboxamides as trpv3 modulators |
| WO2017048702A1 (en) | 2015-09-14 | 2017-03-23 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN107056715B (zh) * | 2017-04-07 | 2019-07-30 | 江南大学 | 一种增强TRPV4-KCa2.3复合体耦联度的化合物及其在抗高血压中的应用 |
| CN110339360B (zh) * | 2018-04-02 | 2024-04-19 | 苏中药业集团股份有限公司 | 瞬时受体电位阳离子通道trpv3在研制预防或治疗银屑病药物中的应用 |
| FR3088823B1 (fr) * | 2018-11-28 | 2020-12-11 | Commissariat Energie Atomique | Nouvelles dihydroquinazolinones ayant une activite protectrice vis-a-vis de toxines au mode d’action intracellulaire, de virus et de bacteries |
| CN113396149B (zh) * | 2018-12-06 | 2024-07-02 | 星座制药公司 | Trex1的调节剂 |
| KR20210129677A (ko) | 2019-02-15 | 2021-10-28 | 노파르티스 아게 | 안구 표면 통증의 치료 방법 |
| JP6994061B2 (ja) | 2019-02-15 | 2022-01-14 | ノバルティス アーゲー | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| MX2021015605A (es) * | 2019-06-27 | 2022-02-16 | Glaxosmithkline Ip Dev Ltd | Compuestos 2,3-dihidroquinazolin como inhibidores nav1.8. |
| EP4003985A1 (en) * | 2019-07-23 | 2022-06-01 | Constellation Pharmaceuticals, Inc. | Modulators of trex1 |
| WO2021154966A1 (en) | 2020-01-29 | 2021-08-05 | Kamari Pharma Ltd. | Compounds and compositions for use in treating skin disorders |
| CN113197900B (zh) * | 2021-01-27 | 2022-07-29 | 徐州医科大学 | Trpml1特异性小分子抑制剂ml-si3的应用 |
| CN116270670A (zh) * | 2023-04-26 | 2023-06-23 | 南通大学 | 化合物2-apb在制备治疗帕金森病药物制剂中的应用 |
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| GB0509573D0 (en) | 2005-05-11 | 2005-06-15 | Merck Sharp & Dohme | Therapeutic compounds |
| US20090298856A1 (en) | 2005-05-11 | 2009-12-03 | Rebecca Elizabeth Brown | 2,3 Substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilliod-1receptor (VR1) |
| US7893260B2 (en) * | 2005-11-04 | 2011-02-22 | Hydra Biosciences, Inc. | Substituted quinazolin-4-one compounds for antagonizing TRPV3 function |
| US7998980B2 (en) | 2006-09-15 | 2011-08-16 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
| WO2008140750A1 (en) * | 2007-05-10 | 2008-11-20 | Hydra Biosciences Inc. | Compounds for modulating trpv3 function |
-
2006
- 2006-11-03 US US11/592,783 patent/US7893260B2/en active Active
- 2006-11-03 TW TW095140730A patent/TWI409070B/zh not_active IP Right Cessation
- 2006-11-03 WO PCT/US2006/042930 patent/WO2007056124A2/en not_active Ceased
- 2006-11-03 CA CA002628441A patent/CA2628441A1/en not_active Abandoned
- 2006-11-03 EP EP06836869A patent/EP1954283A2/en not_active Withdrawn
- 2006-11-03 CN CN2006800496369A patent/CN101355946B/zh not_active Expired - Fee Related
- 2006-11-03 JP JP2008540085A patent/JP2009514954A/ja active Pending
- 2006-11-03 AU AU2006311883A patent/AU2006311883A1/en not_active Abandoned
- 2006-11-03 US US12/084,610 patent/US20100152209A1/en not_active Abandoned
-
2011
- 2011-02-07 US US13/022,107 patent/US8552009B2/en active Active
-
2013
- 2013-08-30 US US14/014,636 patent/US20140155417A1/en not_active Abandoned
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