JP2008509191A5 - - Google Patents
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- Publication number
- JP2008509191A5 JP2008509191A5 JP2007525263A JP2007525263A JP2008509191A5 JP 2008509191 A5 JP2008509191 A5 JP 2008509191A5 JP 2007525263 A JP2007525263 A JP 2007525263A JP 2007525263 A JP2007525263 A JP 2007525263A JP 2008509191 A5 JP2008509191 A5 JP 2008509191A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- compound
- formula
- ethyl group
- naphthalenyl
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims 48
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 17
- 238000000034 method Methods 0.000 claims 14
- 206010020751 Hypersensitivity Diseases 0.000 claims 4
- 208000010668 atopic eczema Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- DHLZHFIJSYWCJK-UHFFFAOYSA-N 1,1,1-trifluoro-2-[(1-methyl-3,4-dihydro-2h-naphthalen-1-yl)methyl]-3-[(2-methylquinolin-5-yl)amino]propan-2-ol Chemical compound C1CCC2=CC=CC=C2C1(C)CC(O)(C(F)(F)F)CNC1=CC=CC2=NC(C)=CC=C21 DHLZHFIJSYWCJK-UHFFFAOYSA-N 0.000 claims 3
- AEYUJQIHDRFOMU-UHFFFAOYSA-N 1,1,1-trifluoro-2-[(isoquinolin-5-ylamino)methyl]-3-(1-methyl-3,4-dihydro-2h-naphthalen-1-yl)propan-2-ol Chemical compound C1CCC2=CC=CC=C2C1(C)CC(O)(C(F)(F)F)CNC1=CC=CC2=CN=CC=C12 AEYUJQIHDRFOMU-UHFFFAOYSA-N 0.000 claims 3
- XJFFZMILSHZEQK-UHFFFAOYSA-N 2-[(1-ethyl-3,4-dihydro-2h-naphthalen-1-yl)methyl]-1,1,1-trifluoro-3-[(2-methylquinolin-5-yl)amino]propan-2-ol Chemical compound C1CCC2=CC=CC=C2C1(CC)CC(O)(C(F)(F)F)CNC1=CC=CC2=NC(C)=CC=C12 XJFFZMILSHZEQK-UHFFFAOYSA-N 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 3
- 238000006243 chemical reaction Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- KXCAEQNNTZANTK-UHFFFAOYSA-N stannane Chemical compound [SnH4] KXCAEQNNTZANTK-UHFFFAOYSA-N 0.000 claims 3
- 229910000080 stannane Inorganic materials 0.000 claims 3
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 3
- IDXIGNMGABVLIG-UHFFFAOYSA-N 1,1,1-trifluoro-2-[(1-methyl-3,4-dihydro-2h-naphthalen-1-yl)methyl]-3-(quinolin-5-ylamino)propan-2-ol Chemical compound C1CCC2=CC=CC=C2C1(C)CC(O)(C(F)(F)F)CNC1=CC=CC2=NC=CC=C12 IDXIGNMGABVLIG-UHFFFAOYSA-N 0.000 claims 2
- CNAHGVBTDVLLSD-UHFFFAOYSA-N 2-[(1-ethyl-3,4-dihydro-2h-naphthalen-1-yl)methyl]-1,1,1-trifluoro-3-(isoquinolin-5-ylamino)propan-2-ol Chemical compound C1CCC2=CC=CC=C2C1(CC)CC(O)(C(F)(F)F)CNC1=CC=CC2=CN=CC=C12 CNAHGVBTDVLLSD-UHFFFAOYSA-N 0.000 claims 2
- 206010027654 Allergic conditions Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 206010012434 Dermatitis allergic Diseases 0.000 claims 2
- XPDWGBQVDMORPB-UHFFFAOYSA-N Fluoroform Chemical compound FC(F)F XPDWGBQVDMORPB-UHFFFAOYSA-N 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 201000009053 Neurodermatitis Diseases 0.000 claims 2
- 208000003251 Pruritus Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 230000007815 allergy Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- CTSLXHKWHWQRSH-UHFFFAOYSA-N oxalyl chloride Chemical compound ClC(=O)C(Cl)=O CTSLXHKWHWQRSH-UHFFFAOYSA-N 0.000 claims 2
- 230000035479 physiological effects, processes and functions Effects 0.000 claims 2
- 239000003380 propellant Substances 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 206010039083 rhinitis Diseases 0.000 claims 2
- 208000017520 skin disease Diseases 0.000 claims 2
- FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 claims 2
- YFMFNYKEUDLDTL-UHFFFAOYSA-N 1,1,1,2,3,3,3-heptafluoropropane Chemical compound FC(F)(F)C(F)C(F)(F)F YFMFNYKEUDLDTL-UHFFFAOYSA-N 0.000 claims 1
- LVGUZGTVOIAKKC-UHFFFAOYSA-N 1,1,1,2-tetrafluoroethane Chemical group FCC(F)(F)F LVGUZGTVOIAKKC-UHFFFAOYSA-N 0.000 claims 1
- GCMNJUJAKQGROZ-UHFFFAOYSA-N 1,2-Dihydroquinolin-2-imine Chemical compound C1=CC=CC2=NC(N)=CC=C21 GCMNJUJAKQGROZ-UHFFFAOYSA-N 0.000 claims 1
- HOGKUWCBDMVMEX-UHFFFAOYSA-N 2-[(1-ethyl-3,4-dihydro-2h-naphthalen-1-yl)methyl]-1,1,1-trifluoro-3-(quinolin-5-ylamino)propan-2-ol Chemical compound C1CCC2=CC=CC=C2C1(CC)CC(O)(C(F)(F)F)CNC1=CC=CC2=NC=CC=C12 HOGKUWCBDMVMEX-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000000048 adrenergic agonist Substances 0.000 claims 1
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- KYKAJFCTULSVSH-UHFFFAOYSA-N chloro(fluoro)methane Chemical compound F[C]Cl KYKAJFCTULSVSH-UHFFFAOYSA-N 0.000 claims 1
- 230000001268 conjugating effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 150000002118 epoxides Chemical class 0.000 claims 1
- NBVXSUQYWXRMNV-UHFFFAOYSA-N fluoromethane Chemical compound FC NBVXSUQYWXRMNV-UHFFFAOYSA-N 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 230000003301 hydrolyzing effect Effects 0.000 claims 1
- OSILBMSORKFRTB-UHFFFAOYSA-N isoquinolin-1-amine Chemical compound C1=CC=C2C(N)=NC=CC2=C1 OSILBMSORKFRTB-UHFFFAOYSA-N 0.000 claims 1
- 150000002825 nitriles Chemical class 0.000 claims 1
- 239000012038 nucleophile Substances 0.000 claims 1
- 150000007530 organic bases Chemical class 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 239000008249 pharmaceutical aerosol Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 claims 1
- 238000005583 trifluoroacetylation reaction Methods 0.000 claims 1
- 0 Nc1cccc2c1C=C**2 Chemical compound Nc1cccc2c1C=C**2 0.000 description 4
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0418045.1A GB0418045D0 (en) | 2004-08-12 | 2004-08-12 | Compounds |
| PCT/EP2005/008763 WO2006015870A1 (en) | 2004-08-12 | 2005-08-10 | Tetrahydro-naphthalene derivatives as glucocorticoid receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008509191A JP2008509191A (ja) | 2008-03-27 |
| JP2008509191A5 true JP2008509191A5 (https=) | 2008-09-18 |
Family
ID=33017436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007525263A Pending JP2008509191A (ja) | 2004-08-12 | 2005-08-10 | グルココルチコイド受容体調節剤としてのテトラヒドロ−ナフタレン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7902224B2 (https=) |
| EP (1) | EP1776119B9 (https=) |
| JP (1) | JP2008509191A (https=) |
| AT (1) | ATE541572T1 (https=) |
| ES (1) | ES2380927T3 (https=) |
| GB (1) | GB0418045D0 (https=) |
| PL (1) | PL1776119T3 (https=) |
| WO (1) | WO2006015870A1 (https=) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7662821B2 (en) | 2003-10-08 | 2010-02-16 | Bayer Schering Pharma Ag | Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents |
| DE502004002403D1 (de) | 2003-10-08 | 2007-02-01 | Schering Ag | Tetrahydronaphthalinderivate, verfahren zu ihrer herstellung und ihre verwendung als entzündungshemmer |
| US7638515B2 (en) | 2003-10-08 | 2009-12-29 | Bayer Schering Pharma Aktiengesellschaft | Tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents |
| US20080153859A1 (en) | 2004-04-05 | 2008-06-26 | Hartmut Rehwinkel | Multiply-substituted tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents |
| DE102004063227A1 (de) * | 2004-12-22 | 2006-07-06 | Schering Ag | Tricylische Aminoalkohole, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| DE102005017301A1 (de) * | 2005-04-14 | 2006-10-19 | Schering Ag | Substituierte Chromanderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| TW200730498A (en) | 2005-12-20 | 2007-08-16 | Glaxo Group Ltd | Compounds |
| EP1834948A1 (de) | 2006-03-15 | 2007-09-19 | Bayer Schering Pharma Aktiengesellschaft | Tetrahydronaphthalinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| MX2008013411A (es) | 2006-04-20 | 2008-11-04 | Glaxo Group Ltd | Nuevos compuestos. |
| GB0611587D0 (en) | 2006-06-12 | 2006-07-19 | Glaxo Group Ltd | Novel compounds |
| PE20081889A1 (es) | 2007-03-23 | 2009-03-05 | Smithkline Beecham Corp | Indol carboxamidas como inhibidores de ikk2 |
| WO2009069736A1 (ja) * | 2007-11-28 | 2009-06-04 | Kyowa Hakko Kirin Co., Ltd. | 含窒素化合物 |
| JP5791500B2 (ja) | 2008-05-23 | 2015-10-07 | パンミラ ファーマシューティカルズ，エルエルシー． | ５−リポキシゲナーゼ活性化タンパク質阻害剤 |
| ES2383246T3 (es) | 2008-06-05 | 2012-06-19 | Glaxo Group Limited | 4-amino-indazoles |
| ES2566339T3 (es) | 2008-06-05 | 2016-04-12 | Glaxo Group Limited | Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas |
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| EP2408458A1 (en) | 2009-03-19 | 2012-01-25 | Merck Sharp&Dohme Corp. | RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 6 (STAT6) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) |
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| JP2012521764A (ja) | 2009-03-27 | 2012-09-20 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸（ｓｉＮＡ）を用いた胸腺間質性リンパ球新生因子（ＴＳＬＰ）遺伝子発現のＲＮＡ干渉媒介性阻害 |
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| US20120004281A1 (en) | 2009-03-27 | 2012-01-05 | Merck Sharp & Dohme Corp | RNA Interference Mediated Inhibition of the Nerve Growth Factor Beta Chain (NGFB) Gene Expression Using Short Interfering Nucleic Acid (siNA) |
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| US10683297B2 (en) | 2017-11-19 | 2020-06-16 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| AU2019209960B2 (en) | 2018-01-20 | 2023-11-23 | Sunshine Lake Pharma Co., Ltd. | Substituted aminopyrimidine compounds and methods of use |
| BR112022019245A2 (pt) | 2020-03-26 | 2022-11-16 | Glaxosmithkline Ip Dev Ltd | Inibidores de catepsina para prevenir ou tratar infecções virais |
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| GB0204719D0 (en) | 2002-02-28 | 2002-04-17 | Glaxo Group Ltd | Medicinal compounds |
| UA80120C2 (en) | 2002-03-26 | 2007-08-27 | Boehringer Ingelheim Pharma | Glucocorticoid mimetics, pharmaceutical composition based thereon |
| DE10215316C1 (de) | 2002-04-02 | 2003-12-18 | Schering Ag | Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer |
| AU2003222841A1 (en) | 2002-04-25 | 2003-11-10 | Glaxo Group Limited | Phenethanolamine derivatives |
| GB0217225D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicinal compounds |
| GB0220730D0 (en) | 2002-09-06 | 2002-10-16 | Glaxo Group Ltd | Medicinal compounds |
| CN100387598C (zh) | 2002-09-16 | 2008-05-14 | 葛兰素集团有限公司 | 吡唑并[3,4-b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途 |
| WO2004037807A2 (en) | 2002-10-22 | 2004-05-06 | Glaxo Group Limited | Medicinal arylethanolamine compounds |
| GB0225030D0 (en) | 2002-10-28 | 2002-12-04 | Glaxo Group Ltd | Medicinal compounds |
| ATE390407T1 (de) | 2002-10-28 | 2008-04-15 | Glaxo Group Ltd | Phenethanolamin-derivate zur behandlung von atemwegserkrankungen |
| GB0225535D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| GB0225540D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| DE10261874A1 (de) | 2002-12-20 | 2004-07-08 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| CA2512257A1 (en) | 2003-01-03 | 2004-07-29 | Boehringer Ingelheim Pharmaceuticals, Inc. | 1-propanol and 1-propylamine derivatives and their use as glucocorticoid ligands |
| WO2004071389A2 (en) | 2003-02-15 | 2004-08-26 | Glaxo Group Limited | Non-steroidal infalmmation inhibitors |
| EP1638945A1 (de) | 2003-07-01 | 2006-03-29 | Schering Aktiengesellschaft | Heterozyklisch substituierte pentanol-derivate, verfahren zu ihrer herstellung und ihre verwendung als entz ndungshemmer |
| UY28526A1 (es) | 2003-09-24 | 2005-04-29 | Boehringer Ingelheim Pharma | Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos |
| ES2388434T3 (es) | 2003-11-03 | 2012-10-15 | Glaxo Group Limited | Dispositivo de administración de fluido |
-
2004
- 2004-08-12 GB GBGB0418045.1A patent/GB0418045D0/en not_active Ceased
-
2005
- 2005-08-10 AT AT05775926T patent/ATE541572T1/de active
- 2005-08-10 US US11/573,301 patent/US7902224B2/en not_active Expired - Fee Related
- 2005-08-10 ES ES05775926T patent/ES2380927T3/es not_active Expired - Lifetime
- 2005-08-10 EP EP05775926A patent/EP1776119B9/en not_active Expired - Lifetime
- 2005-08-10 WO PCT/EP2005/008763 patent/WO2006015870A1/en not_active Ceased
- 2005-08-10 PL PL05775926T patent/PL1776119T3/pl unknown
- 2005-08-10 JP JP2007525263A patent/JP2008509191A/ja active Pending
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