JP2005538123A5 - - Google Patents
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- Publication number
- JP2005538123A5 JP2005538123A5 JP2004526764A JP2004526764A JP2005538123A5 JP 2005538123 A5 JP2005538123 A5 JP 2005538123A5 JP 2004526764 A JP2004526764 A JP 2004526764A JP 2004526764 A JP2004526764 A JP 2004526764A JP 2005538123 A5 JP2005538123 A5 JP 2005538123A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- phenyl
- alkoxy
- heteroaryl
- 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
- 125000001424 substituent group Chemical group 0.000 claims description 80
- 125000001072 heteroaryl group Chemical group 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 47
- 150000002367 halogens Chemical group 0.000 claims description 46
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 43
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 42
- 229910052799 carbon Inorganic materials 0.000 claims description 39
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 22
- -1 monosubstituted phenyl Chemical group 0.000 claims description 20
- 125000003545 alkoxy group Chemical group 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 13
- 125000003118 aryl group Chemical group 0.000 claims description 11
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 5
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims description 5
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 5
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims description 4
- 125000004104 aryloxy group Chemical group 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- SEPPVOUBHWNCAW-FNORWQNLSA-N (E)-4-oxonon-2-enal Chemical compound CCCCCC(=O)\C=C\C=O SEPPVOUBHWNCAW-FNORWQNLSA-N 0.000 claims description 3
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 3
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 229920001577 copolymer Chemical group 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 230000003511 endothelial effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- KKJUPNGICOCCDW-UHFFFAOYSA-N 7-N,N-Dimethylamino-1,2,3,4,5-pentathiocyclooctane Chemical compound CN(C)C1CSSSSSC1 KKJUPNGICOCCDW-UHFFFAOYSA-N 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010048554 Endothelial dysfunction Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 208000007530 Essential hypertension Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010018367 Glomerulonephritis chronic Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 102000008299 Nitric Oxide Synthase Human genes 0.000 claims 1
- 108010021487 Nitric Oxide Synthase Proteins 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 201000001068 Prinzmetal angina Diseases 0.000 claims 1
- 201000003099 Renovascular Hypertension Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 201000004239 Secondary hypertension Diseases 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 208000009325 Variant Angina Pectoris Diseases 0.000 claims 1
- 206010047281 Ventricular arrhythmia Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 229940124558 contraceptive agent Drugs 0.000 claims 1
- 239000003433 contraceptive agent Substances 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000008694 endothelial dysfunction Effects 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000004936 stimulating effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02017585.7 | 2002-08-07 | ||
| EP02017585A EP1388341A1 (en) | 2002-08-07 | 2002-08-07 | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals |
| PCT/EP2003/008102 WO2004014369A1 (en) | 2002-08-07 | 2003-07-24 | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005538123A JP2005538123A (ja) | 2005-12-15 |
| JP2005538123A5 true JP2005538123A5 (https=) | 2006-09-07 |
| JP4778230B2 JP4778230B2 (ja) | 2011-09-21 |
Family
ID=30129193
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004526764A Expired - Fee Related JP4778230B2 (ja) | 2002-08-07 | 2003-07-24 | アシルアミノ−置換複素芳香族化合物および医薬としてのそれらの使用 |
Country Status (10)
| Country | Link |
|---|---|
| EP (2) | EP1388341A1 (https=) |
| JP (1) | JP4778230B2 (https=) |
| AT (1) | ATE388702T1 (https=) |
| AU (1) | AU2003260325A1 (https=) |
| BR (1) | BR0313294A (https=) |
| CA (1) | CA2494298A1 (https=) |
| DE (1) | DE60319711T2 (https=) |
| IL (1) | IL166493A0 (https=) |
| MX (1) | MXPA05000697A (https=) |
| WO (1) | WO2004014369A1 (https=) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8578101A1 (es) * | 2002-08-13 | 2004-05-07 | Warner Lambert Co | Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz |
| CA2531859C (en) | 2003-07-11 | 2013-08-06 | Merck Patent Gesellschaft Mit Beschraenkter Haftung | Benzimidazole derivatives as raf kinase inhibitors |
| EP1568698A1 (en) | 2004-02-27 | 2005-08-31 | Aventis Pharma Deutschland GmbH | Pyrrole-derivatives as factor Xa inhibitors |
| FR2868421B1 (fr) * | 2004-04-01 | 2008-08-01 | Aventis Pharma Sa | Nouveaux benzothiazoles et leur utilisation comme medicaments |
| WO2006038738A1 (ja) * | 2004-10-08 | 2006-04-13 | Takeda Pharmaceutical Company Limited | 受容体機能調節剤 |
| ES2400287T3 (es) * | 2005-03-14 | 2013-04-08 | High Point Pharmaceuticals, Llc | Derivados de benzazol, composiciones y procedimientos de uso como inhibidores de beta-secretasa |
| WO2007017764A2 (en) | 2005-05-18 | 2007-02-15 | Neuraxon, Inc. | Substituted benzimidazole compounds with dual nos inhibitory activity and muopioid agonist activity |
| EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
| EP1741709A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals |
| JP2009503107A (ja) * | 2005-08-04 | 2009-01-29 | アポジー・バイオテクノロジー・コーポレイション | スフィンゴシンキナーゼ阻害剤およびそれらの使用方法 |
| JP5026511B2 (ja) | 2006-05-18 | 2012-09-12 | エフ．ホフマン−ラ ロシュ アーゲー | アデノシンａ２ｂレセプターアンタゴニストとしてのチアゾロ−ピラミジン／ピリジン尿素誘導体 |
| EP1905764A1 (en) | 2006-09-30 | 2008-04-02 | Sanofi-Aventis | Substituted 2-Phenyl-benzimidazoles and their use as pharmaceuticals |
| EP1923062A1 (en) * | 2006-11-16 | 2008-05-21 | sanofi-aventis | Imidazo[2,1-b]thiazoles and their use as pharmaceuticals |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| EP1942104A1 (en) | 2006-12-20 | 2008-07-09 | sanofi-aventis | Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals |
| EP1939180A1 (en) | 2006-12-20 | 2008-07-02 | sanofi-aventis | Heteroarylacrylamides and their use as pharmaceuticals for the stimulation of the expression of endothelial NO synthase |
| EP1939181A1 (en) | 2006-12-27 | 2008-07-02 | sanofi-aventis | Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase |
| EP1964840A1 (en) | 2007-02-28 | 2008-09-03 | sanofi-aventis | Imidazo[1,2-a]pyridines and their use as pharmaceuticals |
| EP1964841A1 (en) | 2007-02-28 | 2008-09-03 | sanofi-aventis | Imidazo[1,2-a]azine and their use as pharmaceuticals |
| JP2010533729A (ja) | 2007-07-17 | 2010-10-28 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物と方法、及びそのための適応 |
| EP2297097A2 (en) * | 2008-06-11 | 2011-03-23 | Irm Llc | Compounds and compositions useful for the treatment of malaria |
| KR101739994B1 (ko) | 2009-04-03 | 2017-05-25 | 에프. 호프만-라 로슈 아게 | 프로판-１-술폰산 ｛３-［５-（４-클로로-페닐）-１Ｈ-피롤로［２，３-ｂ］피리딘-３-카르보닐］-２，４-디플루오로-페닐｝-아미드 조성물 및 그의 용도 |
| WO2010126743A1 (en) | 2009-04-27 | 2010-11-04 | High Point Pharmaceuticals, Llc | SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS β-SECRETASE INHIBITORS |
| US8329724B2 (en) | 2009-08-03 | 2012-12-11 | Hoffmann-La Roche Inc. | Process for the manufacture of pharmaceutically active compounds |
| NZ599866A (en) | 2009-11-06 | 2014-09-26 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| WO2011119465A1 (en) | 2010-03-23 | 2011-09-29 | High Point Pharmaceuticals, Llc | Substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutical compositions, and methods of use as beta-secretase inhibitors |
| KR101911972B1 (ko) | 2011-02-07 | 2018-10-25 | 플렉시콘 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| WO2013104577A1 (en) * | 2012-01-11 | 2013-07-18 | Acesion Pharma Aps | Benzimidazolyl-acetamide derivatives useful as potassium channel modulators |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| AU2013283318B2 (en) | 2012-06-27 | 2017-11-23 | 4Sc Ag | Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and CNS disorders |
| WO2014007228A1 (ja) | 2012-07-03 | 2014-01-09 | 小野薬品工業株式会社 | ソマトスタチン受容体作動活性を有する化合物およびその医薬用途 |
| CN103772376B (zh) * | 2012-10-24 | 2017-01-11 | 中国医学科学院医药生物技术研究所 | 取代的苯并-1,3-杂唑类化合物、其制备方法及用途 |
| CN102993097A (zh) * | 2012-11-09 | 2013-03-27 | 贵州大学 | 吡唑酰胺类化合物及其应用 |
| WO2015143653A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143654A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143652A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| JP6785217B2 (ja) * | 2014-07-31 | 2020-11-18 | インスティチュート パスツール コリア | ２−アミノ−ベンゾイミダゾール誘導体ならびにこれらの５−リポキシゲナーゼおよび／またはプロスタグランジンｅシンターゼ阻害剤としての使用 |
| WO2016161572A1 (en) | 2015-04-08 | 2016-10-13 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| WO2019162323A1 (en) | 2018-02-21 | 2019-08-29 | Boehringer Ingelheim International Gmbh | New benzimidazole compounds and derivatives as egfr inhibitors |
| US12528778B2 (en) | 2019-05-29 | 2026-01-20 | Syngenta Crop Protection Ag | Microbiocidal derivatives |
| JP7590996B2 (ja) | 2019-06-24 | 2024-11-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｅｇｆｒ阻害剤としての新たな大環状化合物および誘導体 |
| JP7412546B2 (ja) * | 2019-10-02 | 2024-01-12 | 克洛索科学公司 | 抗老化遺伝子ｋｌｏｔｈｏの発現を誘導する化合物およびその用途 |
| AU2022214582C1 (en) * | 2021-01-29 | 2025-02-27 | Korea Research Institute Of Chemical Technology | Benzothiazole and benzimidazole derivatives, pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as active ingredient |
| KR102375097B1 (ko) * | 2021-04-01 | 2022-03-17 | 주식회사 클로소사이언스 | 항노화 유전자 klotho의 발현을 유도하는 화합물을 포함하는 퇴행성 신경질환의 예방 또는 치료용 조성물 |
| JP7728030B2 (ja) * | 2021-04-01 | 2025-08-22 | クロトー サイエンシーズ カンパニー リミテッド | 抗老化遺伝子ｋｌｏｔｈｏの発現を誘導する化合物を含む慢性腎疾患の予防または治療用組成物 |
| EP4436568A4 (en) * | 2021-11-23 | 2025-05-21 | Mayo Foundation for Medical Education and Research | Enhancers of particulate guanylyl cyclase receptor a |
| CN115109011B (zh) * | 2022-08-10 | 2023-12-15 | 河北师范大学 | 一种苯并噻唑类化合物、制备方法和用途 |
| CN119330886B (zh) * | 2024-09-03 | 2026-03-20 | 常州大学 | 一种苯并咪唑胺类衍生物及其制备方法和作为β2-肾上腺素受体别构拮抗剂的应用 |
| CN120136812B (zh) * | 2025-03-15 | 2025-09-30 | 昆明医科大学 | 一类靶向降解转录因子klf5的化合物及其应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA71587C2 (uk) * | 1998-11-10 | 2004-12-15 | Шерінг Акцієнгезелльшафт | Аміди антранілової кислоти та їхнє застосування як лікарських засобів |
| WO2001083427A1 (en) * | 2000-04-28 | 2001-11-08 | Sankyo Company, Limited | PPARη MODULATORS |
| MXPA03009130A (es) * | 2000-10-20 | 2004-02-26 | Biocryst Pharm Inc | Compuestos de biarilo que funcionan como inhibidores de proteasa serina. |
| TWI241190B (en) * | 2001-02-13 | 2005-10-11 | Aventis Pharma Gmbh | 4-Fluoro-N-indan-2-yl benzamide and its use as pharmaceutical |
-
2002
- 2002-08-07 EP EP02017585A patent/EP1388341A1/en not_active Withdrawn
-
2003
- 2003-07-24 DE DE60319711T patent/DE60319711T2/de not_active Expired - Lifetime
- 2003-07-24 WO PCT/EP2003/008102 patent/WO2004014369A1/en not_active Ceased
- 2003-07-24 EP EP03784054A patent/EP1534275B1/en not_active Expired - Lifetime
- 2003-07-24 MX MXPA05000697A patent/MXPA05000697A/es not_active Application Discontinuation
- 2003-07-24 AT AT03784054T patent/ATE388702T1/de not_active IP Right Cessation
- 2003-07-24 CA CA002494298A patent/CA2494298A1/en not_active Abandoned
- 2003-07-24 BR BR0313294-3A patent/BR0313294A/pt not_active IP Right Cessation
- 2003-07-24 AU AU2003260325A patent/AU2003260325A1/en not_active Abandoned
- 2003-07-24 JP JP2004526764A patent/JP4778230B2/ja not_active Expired - Fee Related
-
2005
- 2005-01-25 IL IL16649305A patent/IL166493A0/xx unknown
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