JP2004528312A5 - - Google Patents
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- Publication number
- JP2004528312A5 JP2004528312A5 JP2002576207A JP2002576207A JP2004528312A5 JP 2004528312 A5 JP2004528312 A5 JP 2004528312A5 JP 2002576207 A JP2002576207 A JP 2002576207A JP 2002576207 A JP2002576207 A JP 2002576207A JP 2004528312 A5 JP2004528312 A5 JP 2004528312A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- substituted
- hydrogen
- och
- 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 47
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000012458 free base Substances 0.000 claims 9
- 239000002253 acid Substances 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- BJLUORNGPCXNHM-UHFFFAOYSA-N 1H-pyrido[3,2-d]pyrimidine-2,4-dione Chemical compound C1=CN=C2C(=O)NC(=O)NC2=C1 BJLUORNGPCXNHM-UHFFFAOYSA-N 0.000 claims 4
- HYSLHVMRVBBRIG-UHFFFAOYSA-N 6-chloro-2-methyl-1H-pyrido[3,2-d]pyrimidin-4-one Chemical compound C1=C(Cl)N=C2C(=O)NC(C)=NC2=C1 HYSLHVMRVBBRIG-UHFFFAOYSA-N 0.000 claims 4
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 125000006277 halobenzyl group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 102000011040 TRPV Cation Channels Human genes 0.000 claims 2
- 108010062740 TRPV Cation Channels Proteins 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 210000002435 Tendons Anatomy 0.000 claims 1
- 150000008043 acidic salts Chemical group 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 201000005569 gout Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000004595 synovitis Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0107505A GB0107505D0 (en) | 2001-03-26 | 2001-03-26 | Organic compounds |
| GB0107505.0 | 2001-03-26 | ||
| US33828101P | 2001-12-06 | 2001-12-06 | |
| US60/338,281 | 2001-12-06 | ||
| PCT/EP2002/003332 WO2002076946A2 (en) | 2001-03-26 | 2002-03-25 | Fused pyridine derivatives for use as vanilloid receptor antagonists for treating pain. |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004528312A JP2004528312A (ja) | 2004-09-16 |
| JP2004528312A5 true JP2004528312A5 (US07928230-20110419-C00134.png) | 2005-08-04 |
| JP4205430B2 JP4205430B2 (ja) | 2009-01-07 |
Family
ID=26245894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002576207A Expired - Fee Related JP4205430B2 (ja) | 2001-03-26 | 2002-03-25 | 疼痛を治療するための、バニロイド受容体アンタゴニストとして、使用するための縮合ピリジン誘導体 |
Country Status (17)
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE328868T1 (de) | 2000-08-21 | 2006-06-15 | Pacific Corp | Neue (thio)harnstoffverbindungen und arzneimittelkompositionen, die diese enthalten |
| CN100439332C (zh) | 2000-08-21 | 2008-12-03 | 株式会社太平洋 | 硫脲衍生物以及包含该衍生物的药物组合物 |
| MXPA04006882A (es) | 2002-01-17 | 2004-12-06 | Neurogen Corp | Analogos substituidos de quinazolin-4-ilamina como moduladores de receptores de capsaicina. |
| WO2003066595A2 (en) | 2002-02-01 | 2003-08-14 | Euro-Celtique S.A. | 2 - piperazine - pyridines useful for treating pain |
| US6864261B2 (en) | 2002-05-02 | 2005-03-08 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| GB0229808D0 (en) * | 2002-12-20 | 2003-01-29 | Glaxo Group Ltd | Novel compositions |
| US7531558B2 (en) | 2003-02-14 | 2009-05-12 | Glaxo Group Limited | Carboxamide derivatives |
| JP5279987B2 (ja) | 2003-05-20 | 2013-09-04 | 味の素株式会社 | アミド誘導体 |
| GB0319150D0 (en) | 2003-08-14 | 2003-09-17 | Glaxo Group Ltd | Novel compounds |
| JP2007511496A (ja) | 2003-11-14 | 2007-05-10 | メルク シャープ エンド ドーム リミテッド | バニロイド−１受容体（ｖｒ１）の機能を調節する二環式ピリミジン−４−（３ｈ）−オン類並びにその類似体及び誘導体 |
| GB0412769D0 (en) | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| WO2006019965A2 (en) * | 2004-07-16 | 2006-02-23 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| WO2006007851A2 (en) | 2004-07-19 | 2006-01-26 | Novo Nordisk A/S | Capsaicin inhibitors for treating obesity and-related disorders |
| DE102004039373A1 (de) | 2004-08-12 | 2006-02-23 | Grünenthal GmbH | Para-Alkyl-substituierte N-(4-Hydroxy-3-methoxy-benzyl)-zimtsäureamide und deren Verwendung zur Herstellung von Arzneimitteln |
| KR20060087386A (ko) | 2005-01-28 | 2006-08-02 | 주식회사 대웅제약 | 신규 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물 |
| WO2006098554A1 (en) * | 2005-03-16 | 2006-09-21 | Amorepacific Corporation | Novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and a pharmaceutical composition containing the same |
| GB0506147D0 (en) * | 2005-03-24 | 2005-05-04 | Merck Sharp & Dohme | Therapeutic agents |
| 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) |
| KR101347102B1 (ko) * | 2005-10-19 | 2014-01-03 | 그뤼넨탈 게엠베하 | 신규한 바닐로이드 수용체 리간드 및 약제를 제조하기 위한이의 용도 |
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| KR100761222B1 (ko) * | 2006-03-08 | 2007-10-04 | 성균관대학교산학협력단 | 약물의존중독을 예방 및 치료하기 위한 바닐로이드 수용체길항제 |
| GB0614471D0 (en) | 2006-07-20 | 2006-08-30 | Syngenta Ltd | Herbicidal Compounds |
| CN101506210A (zh) | 2006-08-23 | 2009-08-12 | 神经能质公司 | 2-苯氧基嘧啶酮类似物 |
| US20080207659A1 (en) | 2007-02-15 | 2008-08-28 | Asit Kumar Chakraborti | Inhibitors of phosphodiesterase type 4 |
| WO2008129000A1 (en) * | 2007-04-20 | 2008-10-30 | Novartis Ag | Pyridopyrimidine derivatives and use thereof in the treatment of itch and itch related disorders |
| EP2178562B1 (en) | 2007-07-18 | 2017-08-23 | Novartis AG | Synergistic combinations of vr-1 antagonists and cox-2 inhibitors |
| JP5419894B2 (ja) * | 2008-01-11 | 2014-02-19 | グレンマーク ファーマシューティカルズ， エセ．アー． | Ｔｒｐｖ３モジュレーターとしての縮合ピリミジン誘導体 |
| WO2009121036A2 (en) * | 2008-03-27 | 2009-10-01 | Neurogen Corporation | Substituted aryl pyrimidinone derivatives |
| CN101983197B (zh) | 2008-04-18 | 2015-04-22 | 大熊制药株式会社 | 新型苯并噁嗪苯并咪唑衍生物、含有该衍生物的药物组合物及其用途 |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
| AR080055A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1 |
| EP2531490B1 (en) | 2010-02-02 | 2014-10-15 | Novartis AG | Cyclohexyl amide derivatives as crf receptor antagonists |
| KR101293384B1 (ko) | 2010-10-13 | 2013-08-05 | 주식회사 대웅제약 | 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도 |
| US8546416B2 (en) | 2011-05-27 | 2013-10-01 | Novartis Ag | 3-spirocyclic piperidine derivatives as ghrelin receptor agonists |
| EP2852591A1 (en) | 2012-05-03 | 2015-04-01 | Novartis AG | L-malate salt of 2, 7 - diaza - spiro [4.5]dec- 7 - yle derivatives and crystalline forms thereof as ghrelin receptor agonists |
| CN107108429B (zh) | 2015-12-23 | 2022-08-19 | 联邦科学与工业研究组织 | 化合物 |
| CN108863949B (zh) * | 2018-07-09 | 2021-01-15 | 湖南博隽生物医药有限公司 | 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法 |
| DE102022104759A1 (de) | 2022-02-28 | 2023-08-31 | SCi Kontor GmbH | Co-Kristall-Screening Verfahren, insbesondere zur Herstellung von Co-Kristallen |
| CN114605408B (zh) * | 2022-03-30 | 2023-06-16 | 沈阳药科大学 | 5-羟基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制法和应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2749344A (en) * | 1953-01-02 | 1956-06-05 | Burroughs Wellcome Co | Pyrimidine compounds |
| US5958930A (en) * | 1991-04-08 | 1999-09-28 | Duquesne University Of The Holy Ghost | Pyrrolo pyrimidine and furo pyrimidine derivatives |
| JPH09510695A (ja) | 1994-01-03 | 1997-10-28 | エイシア・ファーマシュウティカルズ，インコーポレイテッド | ８−アザ、６−アザ、および６，８−ジアザ−１，４−ジヒドロキノキサリン−２，３−ジオン類およびそのグリシン／ｎｍｄａリセプターに対するアンタゴニストとしての使用 |
| FR2750862B1 (fr) | 1996-07-12 | 1998-10-16 | Dupin Jean Pierre | Utilisation d'heterocycles diazotes fusionnes avec un systeme aromatique ou heteroaromatique pour le traitement des maladies thrombo-emboliques |
-
2002
- 2002-03-25 WO PCT/EP2002/003332 patent/WO2002076946A2/en not_active Application Discontinuation
- 2002-03-25 CA CA002441599A patent/CA2441599A1/en not_active Abandoned
- 2002-03-25 CN CNA028073495A patent/CN1500089A/zh active Pending
- 2002-03-25 RU RU2003130221/04A patent/RU2003130221A/ru not_active Application Discontinuation
- 2002-03-25 HU HU0303623A patent/HUP0303623A2/hu unknown
- 2002-03-25 IL IL15781502A patent/IL157815A0/xx unknown
- 2002-03-25 SK SK1195-2003A patent/SK11952003A3/sk unknown
- 2002-03-25 PL PL02363907A patent/PL363907A1/xx not_active Application Discontinuation
- 2002-03-25 MX MXPA03008754A patent/MXPA03008754A/es not_active Application Discontinuation
- 2002-03-25 KR KR10-2003-7012460A patent/KR20030083755A/ko not_active Application Discontinuation
- 2002-03-25 CZ CZ20032561A patent/CZ20032561A3/cs unknown
- 2002-03-25 BR BR0208338-8A patent/BR0208338A/pt not_active IP Right Cessation
- 2002-03-25 EP EP02730062A patent/EP1377576A2/en not_active Withdrawn
- 2002-03-25 JP JP2002576207A patent/JP4205430B2/ja not_active Expired - Fee Related
- 2002-03-25 US US10/469,756 patent/US7915264B2/en not_active Expired - Fee Related
- 2002-03-26 PE PE2002000241A patent/PE20021161A1/es not_active Application Discontinuation
-
2003
- 2003-09-16 NO NO20034122A patent/NO326546B1/no not_active IP Right Cessation
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