JP2004537541A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2004537541A5 JP2004537541A5 JP2003508914A JP2003508914A JP2004537541A5 JP 2004537541 A5 JP2004537541 A5 JP 2004537541A5 JP 2003508914 A JP2003508914 A JP 2003508914A JP 2003508914 A JP2003508914 A JP 2003508914A JP 2004537541 A5 JP2004537541 A5 JP 2004537541A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- phenyl
- trifluoromethyl
- halo
- 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
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 35
- 125000000217 alkyl group Chemical group 0.000 claims 30
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 20
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000005843 halogen group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- -1 amino, hydroxy Chemical group 0.000 claims 13
- 125000004076 pyridyl group Chemical group 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 claims 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 6
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 5
- 125000001475 halogen functional group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- QCGPNKGBXUZKRV-UHFFFAOYSA-N 3-chloro-1-methyl-5-[(2-phenylbenzoyl)amino]indole-2-carboxylic acid Chemical compound C=1C=C2N(C)C(C(O)=O)=C(Cl)C2=CC=1NC(=O)C1=CC=CC=C1C1=CC=CC=C1 QCGPNKGBXUZKRV-UHFFFAOYSA-N 0.000 claims 1
- UATDNHVWCBSEJH-UHFFFAOYSA-N 3-chloro-1-methyl-n-[2-oxo-1-phenyl-2-(prop-2-ynylamino)ethyl]-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide Chemical compound ClC=1C2=CC(NC(=O)C=3C(=CC=CC=3)C=3C=CC(=CC=3)C(F)(F)F)=CC=C2N(C)C=1C(=O)NC(C(=O)NCC#C)C1=CC=CC=C1 UATDNHVWCBSEJH-UHFFFAOYSA-N 0.000 claims 1
- OLQQRYRTLUMYCV-UHFFFAOYSA-N 3-chloro-1-methyl-n-[2-oxo-1-phenyl-2-(propan-2-ylamino)ethyl]-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide Chemical compound C=1C=CC=CC=1C(C(=O)NC(C)C)NC(=O)C(N(C1=CC=2)C)=C(Cl)C1=CC=2NC(=O)C1=CC=CC=C1C1=CC=C(C(F)(F)F)C=C1 OLQQRYRTLUMYCV-UHFFFAOYSA-N 0.000 claims 1
- KXRBCMNXDPKVMV-UHFFFAOYSA-N 3-chloro-1-methyl-n-[2-oxo-1-phenyl-2-(propylamino)ethyl]-5-[(2-phenylbenzoyl)amino]indole-2-carboxamide Chemical compound C=1C=CC=CC=1C(C(=O)NCCC)NC(=O)C(N(C1=CC=2)C)=C(Cl)C1=CC=2NC(=O)C1=CC=CC=C1C1=CC=CC=C1 KXRBCMNXDPKVMV-UHFFFAOYSA-N 0.000 claims 1
- UWMUBZILFCWRDQ-UHFFFAOYSA-N 3-chloro-1-methyl-n-[2-oxo-1-phenyl-2-(propylamino)ethyl]-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide Chemical compound C=1C=CC=CC=1C(C(=O)NCCC)NC(=O)C(N(C1=CC=2)C)=C(Cl)C1=CC=2NC(=O)C1=CC=CC=C1C1=CC=C(C(F)(F)F)C=C1 UWMUBZILFCWRDQ-UHFFFAOYSA-N 0.000 claims 1
- AXCIWLZUECZEOD-UHFFFAOYSA-N 3-chloro-n-[2-(ethylamino)-2-oxo-1-phenylethyl]-1-methyl-5-[methyl-[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide Chemical compound C=1C=CC=CC=1C(C(=O)NCC)NC(=O)C(N(C1=CC=2)C)=C(Cl)C1=CC=2N(C)C(=O)C1=CC=CC=C1C1=CC=C(C(F)(F)F)C=C1 AXCIWLZUECZEOD-UHFFFAOYSA-N 0.000 claims 1
- FRGXWGKYTCWIOT-UHFFFAOYSA-N C=1C=CC=CC=1C(C(=O)NC(C)C)NC(=O)C(N(C1=CC=2)C)=C(Cl)C1=CC=2N(C)C(=O)C1=CC=CC=C1C1=CC=C(C(F)(F)F)C=C1 Chemical compound C=1C=CC=CC=1C(C(=O)NC(C)C)NC(=O)C(N(C1=CC=2)C)=C(Cl)C1=CC=2N(C)C(=O)C1=CC=CC=C1C1=CC=C(C(F)(F)F)C=C1 FRGXWGKYTCWIOT-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 150000001602 bicycloalkyls Chemical group 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30164401P | 2001-06-28 | 2001-06-28 | |
| PCT/IB2002/001876 WO2003002533A1 (en) | 2001-06-28 | 2002-05-24 | Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (mtp) and/or apolipoprotein b (apo b) secretion |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004537541A JP2004537541A (ja) | 2004-12-16 |
| JP2004537541A5 true JP2004537541A5 (enExample) | 2005-08-18 |
| JP4139325B2 JP4139325B2 (ja) | 2008-08-27 |
Family
ID=23164253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003508914A Expired - Lifetime JP4139325B2 (ja) | 2001-06-28 | 2002-05-24 | ミクロソーム・トリグリセリド・トランスファータンパク質（ｍｔｐ）及び／又はアポリポタンパク質ｂ（ａｐｏｂ）分泌の阻害剤としてのトリアミド置換インドール、ベンゾフラン及びベンゾチオフェン |
Country Status (46)
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60144284D1 (de) | 2000-11-01 | 2011-05-05 | Millennium Pharm Inc | Stickstoffhaltige heterozyklische verbindungen und verfahren zu deren herstellung |
| PL367680A1 (en) * | 2001-06-28 | 2005-03-07 | Pfizer Products Inc. | Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (mtp) and/or apolipoprotein b (apo b) secretion |
| US20030124194A1 (en) * | 2002-01-02 | 2003-07-03 | Gaw Debra A. | Amine functionalized superparamagnetic nanoparticles for the synthesis of bioconjugates and uses therefor |
| CA2515368A1 (en) * | 2003-02-13 | 2004-08-26 | Luciano Rossetti | Regulation of food intake and glucose production by modulation of long-chain fatty acyl-coa levels in the hypothalamus |
| AU2004249123A1 (en) * | 2003-05-20 | 2004-12-29 | Erimos Pharmaceuticals Llc | Methods and compositions for delivery of catecholic butanes for treatment of obesity |
| WO2004111652A1 (en) | 2003-06-19 | 2004-12-23 | Applied Research Systems Ars Holding N.V. | Use of prion conversion modulating agents |
| MXPA06005489A (es) * | 2003-11-14 | 2006-08-11 | Pfizer Prod Inc | Dispersiones de solidos amorfos de un inhibidor de la mtp para el tratamiento de obesidad. |
| CA2555133A1 (en) | 2004-02-04 | 2005-09-01 | Pfizer Products Inc. | Substituted quinoline compounds |
| CA2910191C (en) | 2004-03-05 | 2022-03-08 | The Trustees Of The Univeristy Of Pennsylvania | The use of mtp inhibitors for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side effects |
| FR2873694B1 (fr) * | 2004-07-27 | 2006-12-08 | Merck Sante Soc Par Actions Si | Nouveaux aza-indoles inhibiteurs de la mtp et apob |
| WO2006041922A2 (en) * | 2004-10-08 | 2006-04-20 | Dara Biosciences, Inc. | Agents and methods for administration to the central nervous system |
| PA8660701A1 (es) | 2005-02-04 | 2006-09-22 | Pfizer Prod Inc | Agonistas de pyy y sus usos |
| US20070026079A1 (en) * | 2005-02-14 | 2007-02-01 | Louis Herlands | Intranasal administration of modulators of hypothalamic ATP-sensitive potassium channels |
| EP1890767A2 (en) * | 2005-05-27 | 2008-02-27 | Pfizer Products Inc. | Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss |
| DE102005027274A1 (de) * | 2005-06-08 | 2006-12-14 | Schering Ag | Inhibitoren der löslichen Adenylatzyklase |
| US7417066B2 (en) | 2005-06-08 | 2008-08-26 | Schering Ag | Inhibitors of soluble adenylate cyclase |
| EP1912968A1 (en) * | 2005-08-04 | 2008-04-23 | Pfizer Limited | Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds |
| CA2626441A1 (en) * | 2005-10-18 | 2007-04-26 | Aegerion Pharmaceuticals | Methods for treating disorders associated with hyperlipidemia in a mammal |
| US7741317B2 (en) | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| WO2007061862A2 (en) * | 2005-11-18 | 2007-05-31 | Janssen Pharmaceutica N.V. | 2-keto-oxazoles as modulators of fatty acid amide hydrolase |
| US7888376B2 (en) | 2005-11-23 | 2011-02-15 | Bristol-Myers Squibb Company | Heterocyclic CETP inhibitors |
| WO2007136413A2 (en) | 2005-12-22 | 2007-11-29 | Visen Medical, Inc. | Biocompatible fluorescent metal oxide nanoparticles |
| US8383660B2 (en) | 2006-03-10 | 2013-02-26 | Pfizer Inc. | Dibenzyl amine compounds and derivatives |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| NZ596889A (en) | 2006-04-07 | 2013-06-28 | Vertex Pharma | Use of amide indole derivatives as modulators of ATP-binding cassette transporters |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| JP2010509392A (ja) | 2006-11-13 | 2010-03-25 | ファイザー・プロダクツ・インク | ジアリール、ジピリジニルおよびアリール−ピリジニル誘導体ならびにその使用 |
| US8404896B2 (en) | 2006-12-01 | 2013-03-26 | Bristol-Myers Squibb Company | N-((3-benzyl)-2,2-(bis-phenyl)-propan-1-amine derivatives as CETP inhibitors for the treatment of atherosclerosis and cardiovascular diseases |
| US20080161279A1 (en) * | 2006-12-21 | 2008-07-03 | Wisler Gerald L | Methods of Treating Obesity |
| JP5643514B2 (ja) | 2007-02-09 | 2014-12-17 | ビセン メディカル， インコーポレイテッド | ポリシクロ染料およびその使用 |
| WO2008100423A1 (en) * | 2007-02-09 | 2008-08-21 | Sirtris Pharmaceuticals, Inc. | Gut microsomal triglyceride transport protein inhibitors |
| EP2520561B1 (en) | 2007-06-08 | 2016-02-10 | MannKind Corporation | IRE-1A Inhibitors |
| WO2009014674A1 (en) * | 2007-07-23 | 2009-01-29 | Sirtris Pharmaceuticals, Inc. | Heterocyclylamides as gut microsomal triglyceride transport protein inhibitors |
| CA2710815A1 (en) * | 2008-01-16 | 2009-07-23 | Janssen Pharmaceutica Nv | Combination of metformin and an mtp inhibitor |
| US20090197947A1 (en) * | 2008-02-01 | 2009-08-06 | The Research Foundation Of State University Of New York | Medicaments and methods for lowering plasma lipid levels and screening drugs |
| JP5711151B2 (ja) * | 2010-01-06 | 2015-04-30 | 武田薬品工業株式会社 | インドール誘導体 |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| RU2745977C2 (ru) | 2010-04-22 | 2021-04-05 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения циклоалкилкарбоксамидо-индольных соединений |
| WO2012099785A2 (en) * | 2011-01-20 | 2012-07-26 | The Regents Of The University Of Colorado, A Body Corporate | Modulators of tlr3/dsrna complex and uses thereof |
| CN102108070B (zh) * | 2011-01-26 | 2013-05-22 | 上海优贝德生物医药有限公司 | 5-氨基苯并呋喃-2-甲酸酯及其中间体的制备方法 |
| AU2013290444B2 (en) | 2012-07-16 | 2018-04-26 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof |
| JP6278472B2 (ja) | 2013-02-27 | 2018-02-14 | 塩野義製薬株式会社 | Ａｍｐｋ活性化作用を有するインドールおよびアザインドール誘導体 |
| US9624172B2 (en) | 2014-02-17 | 2017-04-18 | Hetero Research Foundation | Polymorphs of lomitapide and its salts |
| CN103880797B (zh) * | 2014-03-26 | 2015-12-02 | 沈阳大学 | 苯并呋喃类化合物及其医药用途 |
| SG10201913575VA (en) | 2014-04-15 | 2020-02-27 | Vertex Pharma | Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases |
| EP3798214B1 (en) | 2014-10-06 | 2022-09-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP3436446B1 (en) | 2016-03-31 | 2023-06-07 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| SG10201913595YA (en) | 2016-09-30 | 2020-02-27 | Vertex Pharma | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| MA49235B1 (fr) | 2016-12-09 | 2021-02-26 | Vertex Pharma | Modulateur de régulateur de conductance transmembranaire de fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur |
| EP3634402B1 (en) | 2017-06-08 | 2026-01-21 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
| TWI799435B (zh) | 2017-08-02 | 2023-04-21 | 美商維泰克斯製藥公司 | 製備化合物之製程 |
| IL273831B2 (en) | 2017-10-19 | 2024-10-01 | Vertex Pharma | Crystalline forms and compositions of cftr modulators |
| CN111757874B (zh) | 2017-12-08 | 2024-03-08 | 弗特克斯药品有限公司 | 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法 |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| CA3186856A1 (en) | 2020-07-29 | 2022-02-03 | Ruth NALLEN | Lomitapide for use in methods of treating hyperlipidemia and hypercholesterolemia in pediatric patients |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| CN112608271A (zh) * | 2020-11-26 | 2021-04-06 | 安润医药科技（苏州）有限公司 | 酰胺衍生物及其在制备ep4受体拮抗剂中的应用 |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4022900A (en) | 1970-09-09 | 1977-05-10 | Marion Laboratories, Inc. | Compositions containing 1,2,3,4-tetrahydroisoquinolines used as hypotensive agents |
| US4397855A (en) | 1981-06-26 | 1983-08-09 | Warner-Lambert Company | 4-(Substituted)-α, α-dimethyl-1-piperazine pentanoic acids and derivatives as anti-arteriosclerotic agents and method |
| US4647576A (en) * | 1984-09-24 | 1987-03-03 | Warner-Lambert Company | Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis |
| US5416009A (en) | 1991-01-23 | 1995-05-16 | The United States Of America | Nucleotide molecule encoding a specific Onchocerca volvulus antigen for the immunodiagnosis of onchocerciasis |
| US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| HU218419B (hu) | 1992-03-06 | 2000-08-28 | E.R. Squibb And Sons, Inc. | Mikroszomális triglicerid transzfer protein (MTP) nagy molekulatömegű alegységének rekombináns úton történő előállítására és a protein és inhibitorainak kimutatására szolgáló eljárások |
| GB9225141D0 (en) | 1992-12-01 | 1993-01-20 | Smithkline Beecham Corp | Chemical compounds |
| US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| FR2723739B1 (fr) * | 1994-08-19 | 1997-02-14 | Sanofi Sa | Derives de glycinamide, procedes pour leur preparation et medicaments les contenant. |
| EP0832069B1 (en) * | 1995-06-07 | 2003-03-05 | Pfizer Inc. | BIPHENYL-2-CARBOXYLIC ACID-TETRAHYDRO-ISOQUINOLIN-6-YL AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND/OR APOLIPOPROTEIN B (Apo B) SECRETION |
| MX9709914A (es) | 1995-06-07 | 1998-03-31 | Pfizer | Derivados de acido bifenil-2-carboxilico-tetrahidro-isoquinolin-6-ilo, su preparacion y el uso de los mismos. |
| EP1181954A3 (en) | 1995-06-07 | 2002-08-21 | Pfizer Inc. | Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivatives, their preparation and use as inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (ApoB) secretion |
| CA2244729C (en) | 1996-02-02 | 2005-08-23 | Merritt, Brigitte | Device for processing a strand of plastic material |
| US5827875A (en) | 1996-05-10 | 1998-10-27 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| YU23499A (sh) | 1996-11-27 | 2001-07-10 | Pfizer Inc. | Inhibitorski amidi apo-b-sekrecije/mtp-a |
| WO1998027979A1 (en) | 1996-12-20 | 1998-07-02 | Bristol-Myers Squibb Company | Heterocyclic inhibitors of microsomal triglyceride transfer protein and method |
| US6066653A (en) | 1997-01-17 | 2000-05-23 | Bristol-Myers Squibb Co. | Method of treating acid lipase deficiency diseases with an MTP inhibitor and cholesterol lowering drugs |
| US5968950A (en) | 1997-06-23 | 1999-10-19 | Pfizer Inc | Apo B-secretion/MTP inhibitor hydrochloride salt |
| TW460478B (en) * | 1997-08-15 | 2001-10-21 | Chugai Pharmaceutical Co Ltd | Phenethylamine derivatives |
| JP2959765B2 (ja) | 1997-12-12 | 1999-10-06 | 日本たばこ産業株式会社 | ３−ピペリジル−４−オキソキナゾリン誘導体及びそれを含有してなる医薬組成物 |
| PT1042287E (pt) | 1997-12-24 | 2005-08-31 | Aventis Pharma Gmbh | Derivados de indole como inibidores do factor xa |
| EP1080724A4 (en) | 1998-05-22 | 2004-06-23 | Nippon Shinyaku Co Ltd | COMPOSITIONS FOR REDUCING MTP ACTIVITY |
| EP1085846A2 (en) | 1998-06-08 | 2001-03-28 | Advanced Medicine, Inc. | Multibinding inhibitors of microsomal triglyceride transferase protein |
| US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
| CO5090829A1 (es) * | 1998-07-21 | 2001-10-30 | Novartis Ag | Compuestos organicos de la formula i, utiles como inhibido res de la proteina de transferencia de triglicerido microso mal y de la secrecion de la apolipoproteina b. |
| ES2248084T3 (es) * | 1999-06-14 | 2006-03-16 | Eli Lilly And Company | Inhibidores de serinproteasa. |
| DE19933926A1 (de) | 1999-07-20 | 2001-01-25 | Boehringer Ingelheim Pharma | Biphenylderivate, ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE19945594A1 (de) | 1999-09-23 | 2001-03-29 | Boehringer Ingelheim Pharma | Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel |
| CA2325358C (en) * | 1999-11-10 | 2005-08-02 | Pfizer Products Inc. | 7-¬(4'-trifluoromethyl-biphenyl-2-carbonyl)amino|-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein b |
| DE19963235A1 (de) | 1999-12-27 | 2001-07-05 | Boehringer Ingelheim Pharma | Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE19963234A1 (de) | 1999-12-27 | 2002-01-24 | Boehringer Ingelheim Pharma | Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel |
| EP1259484B1 (en) | 2000-01-18 | 2005-05-18 | Novartis AG | Carboxamides useful as inhibitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion |
| WO2001077077A1 (en) | 2000-04-10 | 2001-10-18 | Novartis Ag | Substituted (hetero)aryl carboxamide derivatives as microsomal triglyceride transfer protein (mtp) and apolipoprotein b (apo b) secretion |
| GB0013378D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Use of therapeutic benzamide derivatives |
| GB0013346D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Therapeutic benzamide derivatives |
| GB0013383D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Therapeutic benzamide derivatives |
| DE10033337A1 (de) | 2000-07-08 | 2002-01-17 | Boehringer Ingelheim Pharma | Biphenylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
| US20020032238A1 (en) | 2000-07-08 | 2002-03-14 | Henning Priepke | Biphenylcarboxylic acid amides, the preparation thereof and the use thereof as medicaments |
| FR2816940A1 (fr) | 2000-11-23 | 2002-05-24 | Lipha | Derives de 4-(biphenylcarbonylamino)-piperidine, compositions les contenant et leur utilisation |
| GB0109287D0 (en) | 2001-04-12 | 2001-05-30 | Glaxo Group Ltd | Therapeutic benzamide derivatives |
| PL367680A1 (en) * | 2001-06-28 | 2005-03-07 | Pfizer Products Inc. | Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (mtp) and/or apolipoprotein b (apo b) secretion |
| CN101838218A (zh) | 2002-02-28 | 2010-09-22 | 日本烟草产业株式会社 | 酯化合物及其医药用途 |
-
2002
- 2002-05-24 PL PL02367680A patent/PL367680A1/xx unknown
- 2002-05-24 AU AU2002307839A patent/AU2002307839B2/en not_active Ceased
- 2002-05-24 EA EA200301310A patent/EA007008B1/ru not_active IP Right Cessation
- 2002-05-24 CN CN028130219A patent/CN1522246B/zh not_active Expired - Fee Related
- 2002-05-24 CN CN2006100941142A patent/CN1880304B/zh not_active Expired - Fee Related
- 2002-05-24 HR HR20031051A patent/HRP20031051B1/xx not_active IP Right Cessation
- 2002-05-24 RS YUP-1004/03A patent/RS50712B/sr unknown
- 2002-05-24 MX MXPA03011707A patent/MXPA03011707A/es active IP Right Grant
- 2002-05-24 EE EEP200400040A patent/EE05452B1/xx not_active IP Right Cessation
- 2002-05-24 UA UA20031212657A patent/UA75660C2/uk unknown
- 2002-05-24 KR KR1020037017167A patent/KR100575919B1/ko not_active Expired - Fee Related
- 2002-05-24 HU HU0400348A patent/HU229551B1/hu not_active IP Right Cessation
- 2002-05-24 OA OA1200300327A patent/OA12626A/en unknown
- 2002-05-24 EP EP02780923A patent/EP1404653B1/en not_active Expired - Lifetime
- 2002-05-24 SI SI200230732T patent/SI1404653T1/sl unknown
- 2002-05-24 AT AT02780923T patent/ATE405548T1/de active
- 2002-05-24 PT PT02780923T patent/PT1404653E/pt unknown
- 2002-05-24 BR BR0210616-7A patent/BR0210616A/pt active Search and Examination
- 2002-05-24 GE GE5350A patent/GEP20053720B/en unknown
- 2002-05-24 IL IL15851602A patent/IL158516A0/xx not_active IP Right Cessation
- 2002-05-24 CZ CZ20033558A patent/CZ20033558A3/cs unknown
- 2002-05-24 CA CA002451474A patent/CA2451474C/en not_active Expired - Fee Related
- 2002-05-24 SK SK1610-2003A patent/SK287806B6/sk not_active IP Right Cessation
- 2002-05-24 GE GEAP20027236A patent/GEP20063720B/en unknown
- 2002-05-24 DK DK02780923T patent/DK1404653T3/da active
- 2002-05-24 KR KR1020057025027A patent/KR100575944B1/ko not_active Expired - Fee Related
- 2002-05-24 TN TNPCT/IB2002/001876A patent/TNSN03146A1/fr unknown
- 2002-05-24 WO PCT/IB2002/001876 patent/WO2003002533A1/en not_active Ceased
- 2002-05-24 JP JP2003508914A patent/JP4139325B2/ja not_active Expired - Lifetime
- 2002-05-24 ES ES02780923T patent/ES2307799T3/es not_active Expired - Lifetime
- 2002-05-24 DE DE60228447T patent/DE60228447D1/de not_active Expired - Lifetime
- 2002-05-24 NZ NZ528752A patent/NZ528752A/en not_active IP Right Cessation
- 2002-06-20 US US10/177,858 patent/US6720351B2/en not_active Expired - Fee Related
- 2002-06-21 TW TW094146513A patent/TW200628447A/zh unknown
- 2002-06-21 TW TW091113664A patent/TWI313264B/zh not_active IP Right Cessation
- 2002-06-26 MY MYPI20022415A patent/MY129328A/en unknown
- 2002-06-26 AR ARP020102408A patent/AR036158A1/es active IP Right Grant
- 2002-06-27 GT GT200200136A patent/GT200200136A/es unknown
- 2002-06-27 AP APAP/P/2002/002567A patent/AP1649A/en active
- 2002-06-27 PE PE2002000580A patent/PE20030135A1/es not_active Application Discontinuation
- 2002-06-27 UY UY27360A patent/UY27360A1/es unknown
- 2002-06-28 PA PA20028549301A patent/PA8549301A1/es unknown
-
2003
- 2003-08-13 US US10/639,854 patent/US6979692B2/en not_active Expired - Fee Related
- 2003-08-13 US US10/639,855 patent/US6949572B2/en not_active Expired - Fee Related
- 2003-10-07 ZA ZA200307818A patent/ZA200307818B/en unknown
- 2003-10-09 IS IS6988A patent/IS2603B/is unknown
- 2003-11-17 CR CR7151A patent/CR7151A/es not_active Application Discontinuation
- 2003-12-16 NO NO20035607A patent/NO326700B1/no not_active IP Right Cessation
- 2003-12-22 BG BG108487A patent/BG108487A/bg unknown
- 2003-12-22 MA MA27457A patent/MA27045A1/fr unknown
- 2003-12-23 EC EC2003004925A patent/ECSP034925A/es unknown
-
2005
- 2005-08-02 US US11/196,563 patent/US7482368B2/en not_active Expired - Fee Related
-
2006
- 2006-02-10 US US11/351,571 patent/US7348355B2/en not_active Expired - Fee Related
-
2008
- 2008-10-13 CY CY20081101126T patent/CY1108407T1/el unknown