PE20030135A1 - Derivados indol sustituido con triamida como inhibidores de la secrecion de mtp - Google Patents
Derivados indol sustituido con triamida como inhibidores de la secrecion de mtpInfo
- Publication number
- PE20030135A1 PE20030135A1 PE2002000580A PE2002000580A PE20030135A1 PE 20030135 A1 PE20030135 A1 PE 20030135A1 PE 2002000580 A PE2002000580 A PE 2002000580A PE 2002000580 A PE2002000580 A PE 2002000580A PE 20030135 A1 PE20030135 A1 PE 20030135A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- inhibitors
- phenyl
- triamide
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 230000028327 secretion Effects 0.000 title abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- 229940054051 antipsychotic indole derivative Drugs 0.000 title 1
- 150000001875 compounds Chemical group 0.000 abstract 3
- -1 NITRO, AZIDO, AMINO Chemical class 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 208000035150 Hypercholesterolemia Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000003228 microsomal effect Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Furan Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
COMPUESTOS HETEROBICICLICOS SUSTITUIDOS CON TRIANIDA DE FORMULA Ib DONDE R1 ESTA SUSTITUIDO EN LA POSICION 5 O 6 Y TIENE LA ESTRUCTURA a DONDE R7 ES FENILO, PIRIDILO, FENIL-Z1- PIRIDIL-Z1 CON UNO A CINCO R12; R1 ES ALQUILO C1-C6, CICLOALQUILO C3-C8, BICICLOALQUILO C5-C10, ENTRE OTROS; m ES 0-5; n ES 0-3; p ES 0-3: L ES -C(O)N(R9)-; X1 ES N(R4), S,O; X2 ESN,C(Rc); R2, R8, R11, R12, R13, R16 SON HALO, CIANO, NITRO, AZIDO, AMINO, OH, ENTRE OTROS. R3 ES H, HALO, ALQUILO C1-C6, ENTRE OTROS; R4 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS; r ES 2-5; t ES 1-6; R5 Y R9 SON H, ALQUILO C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS; R6 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS; R7 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R10 ES FENILO, PIRIDILO, ENTRE OTROS; Z2 ES -S(O)j-, -O-, ENTRE OTROS. UN COMPUESTO PREFERIDO ES (2-METILAMINO-2-OXO-FENILETIL)AMIDA DEL ACIDO 1-METIL-5-[(6-METIL-4'-TRIFLUOROMETIL-BIFENIL-2-CARBONIL)-AMINO]-1H-INDOL-2-CARBOXILICO, ENTRE OTROS. SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES DE LA SECRECION DE LA PROTEINA DE TRANSFERENCIA DE TRIGICERIDOS MICROSOMAL (MTP) Y SON UTILES PARA EL TRATAMIENTO DE OBESIDAD, HIPERCOLESTEROLEMIA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30164401P | 2001-06-28 | 2001-06-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20030135A1 true PE20030135A1 (es) | 2003-03-03 |
Family
ID=23164253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002000580A PE20030135A1 (es) | 2001-06-28 | 2002-06-27 | Derivados indol sustituido con triamida como inhibidores de la secrecion de mtp |
Country Status (46)
Families Citing this family (59)
| 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 |
| SI1404653T1 (sl) * | 2001-06-28 | 2008-12-31 | Pfizer Prod Inc | S triamidom substituirani indoli, benzofurani in benzotiofeni kot zaviralci mikrosomske prenašalnebeljakovine za trigliceride (MTP) in/ali izločanja apolipoproteina B (APO B) |
| AU2003207438A1 (en) * | 2002-01-02 | 2003-07-24 | Visen Medical, Inc. | Amine functionalized superparamagnetic nanoparticles for the synthesis of bioconjugates and uses therefor |
| JP2006519229A (ja) * | 2003-02-13 | 2006-08-24 | アルバート・アインシュタイン・カレッジ・オヴ・メディシン・オヴ・イェシヴァ・ユニヴァーシティ | 視床下部内の長鎖脂肪アシルＣｏＡレベルの変調による摂食量およびグルコース産生量の調節 |
| EP1631270A4 (en) * | 2003-05-20 | 2007-11-14 | Erimos Pharmaceutical Llp | METHOD AND COMPOSITIONS FOR DISTRIBUTING CATECHOLIC BUTANES FOR THE TREATMENT OF DISEASES |
| US7598046B2 (en) | 2003-06-19 | 2009-10-06 | Laboratories Serono Sa | Use of prion conversion modulating agents |
| EP1696887A1 (en) * | 2003-11-14 | 2006-09-06 | Pfizer Products Inc. | Solid amorphous dispersions of an mtp inhibitor for treatment of obesity |
| JP2007520543A (ja) | 2004-02-04 | 2007-07-26 | ファイザー・プロダクツ・インク | 置換キノリン化合物 |
| 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 |
| WO2006088875A2 (en) * | 2005-02-14 | 2006-08-24 | Albert Einstein College Of Medicine Of Yeshiva University | Intranasal administration of modulators of hypothalamic atp-sensitive potassium channels |
| JP2008542255A (ja) * | 2005-05-27 | 2008-11-27 | ファイザー・プロダクツ・インク | 肥満症の治療または体重減量の維持のためのカンナビノイド−１受容体アンタゴニストおよびミクロソームトリグリセリド輸送タンパク質阻害物質の併用 |
| US7417066B2 (en) | 2005-06-08 | 2008-08-26 | Schering Ag | Inhibitors of soluble adenylate cyclase |
| DE102005027274A1 (de) * | 2005-06-08 | 2006-12-14 | Schering Ag | Inhibitoren der löslichen Adenylatzyklase |
| WO2007015162A1 (en) * | 2005-08-04 | 2007-02-08 | Pfizer Limited | Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds |
| JP2009511634A (ja) * | 2005-10-18 | 2009-03-19 | エージェリオン ファーマシューティカルズ | 哺乳動物において高脂血症に関連する障害を治療する方法 |
| US7741317B2 (en) | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| EP1954137A4 (en) * | 2005-11-18 | 2008-12-17 | Janssen Pharmaceutica Nv | 2-KETO-OXAZOLE AS MODULATORS OF FATTY ACID AMIDHYDROLASE |
| 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 |
| PT2674428T (pt) * | 2006-04-07 | 2016-07-14 | Vertex Pharma | Modeladores de transportadores de cassetes de ligação de atp |
| 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 |
| EP2084127A1 (en) | 2006-11-13 | 2009-08-05 | Pfizer Products Inc. | Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof |
| 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 |
| AU2007338625A1 (en) * | 2006-12-21 | 2008-07-03 | Aegerion Pharmaceuticals, Inc. | Methods for treating obesity with a combination comprising a MTP inhibitor and a cholesterol absorption inhibitor |
| US20080249130A1 (en) * | 2007-02-09 | 2008-10-09 | Sirtris Pharmaceuticals, Inc. | Gut microsomal triglyceride transport protein inhibitors |
| 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 |
| ES2601856T3 (es) | 2007-06-08 | 2017-02-16 | Mannkind Corporation | Inhibidores de la IRE-1A |
| 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 |
| US8642770B2 (en) * | 2010-01-06 | 2014-02-04 | Takeda Pharmaceutical Company Limited | Indole derivative |
| 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 |
| ES2858351T3 (es) | 2010-04-22 | 2021-09-30 | Vertex Pharma | Compuesto intermedio para proceso de producción de compuestos de cicloalquilcaraboxamido-indol |
| US9409880B2 (en) * | 2011-01-20 | 2016-08-09 | 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 |
| HK1209318A1 (en) | 2012-07-16 | 2016-04-01 | 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 |
| US9890119B2 (en) | 2013-02-27 | 2018-02-13 | Shionogi & Co., Ltd. | Indole and azaindole derivative having AMPK-activating activity |
| EP3107540A4 (en) * | 2014-02-17 | 2017-08-30 | 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 |
| HUE055369T2 (hu) | 2014-04-15 | 2021-11-29 | Vertex Pharma | Gyógyászati készítmények cisztás fibrózis transzmembrán konduktancia regulátor kövzetítette betegségek kezelésére |
| MX2017004543A (es) | 2014-10-06 | 2017-10-04 | Vertex Pharma | Moduladores de regulador de conductancia transmembranal de fibrosis quística. |
| WO2017173274A1 (en) | 2016-03-31 | 2017-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| SMT202100646T1 (it) | 2016-09-30 | 2022-01-10 | Vertex Pharma | Modulatori di regolatore di conduttanza transmembrana della fibrosi cistica, composizioni farmaceutiche, metodi di trattamento, e procedimento per preparare il modulatore |
| HRP20201946T1 (hr) | 2016-12-09 | 2021-01-22 | Vertex Pharmaceuticals Incorporated | Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora |
| EP3634402A1 (en) | 2017-06-08 | 2020-04-15 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| MA49631A (fr) | 2017-07-17 | 2020-05-27 | Vertex Pharma | Méthodes de traitement de la fibrose kystique |
| WO2019028228A1 (en) | 2017-08-02 | 2019-02-07 | Vertex Pharmaceuticals Incorporated | PROCESSES FOR THE PREPARATION OF PYRROLIDINE COMPOUNDS |
| EP3697774B1 (en) | 2017-10-19 | 2025-09-24 | Vertex Pharmaceuticals Incorporated | Crystalline forms and compositions of cftr modulators |
| MA51039A (fr) | 2017-12-08 | 2020-10-14 | Vertex Pharma | Procédés pour préparer des modulateurs du régulateur de la conductance transmembranaire de la mucoviscidose |
| 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 |
| WO2019200246A1 (en) | 2018-04-13 | 2019-10-17 | Alexander Russell Abela | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| 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. |
| US5919795A (en) | 1995-06-07 | 1999-07-06 | 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 |
| PT832069E (pt) | 1995-06-07 | 2003-06-30 | Pfizer | Derivados de tetrahidro-isoquinolin-6-il amida do acido bifenilo-2-carboxilico sua preparacao e sua utilizacao como inibidores de proteina de transferencia de triglicerido microsomal e/ou da secrecao de apolipoproteina b (apo b) |
| WO1996040640A1 (en) * | 1995-06-07 | 1996-12-19 | 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 |
| JP2000505360A (ja) | 1996-02-02 | 2000-05-09 | ブリギッテ メリット | 塑性的な材料から成るストランドを加工するための装置 |
| US5827875A (en) | 1996-05-10 | 1998-10-27 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| NZ335162A (en) | 1996-11-27 | 2000-01-28 | Pfizer | Apo b-secretion/mtp inhibitory amides |
| AU5513298A (en) | 1996-12-20 | 1998-07-17 | 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 |
| ES2241194T3 (es) | 1997-12-24 | 2005-10-16 | Aventis Pharma Deutschland Gmbh | Derivados de indol en calidad de inhibidores de factor xa. |
| AU3170699A (en) | 1998-05-22 | 1999-12-13 | Nippon Shinyaku Co. Ltd. | Mtp activity-lowering compositions |
| CA2319495A1 (en) | 1998-06-08 | 1999-12-16 | Advanced Medicine, Inc. | Multibinding inhibitors of microsomal triglyceride transferase protein |
| 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. |
| US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
| DE60022508T2 (de) * | 1999-06-14 | 2006-06-08 | Eli Lilly And Co., Indianapolis | Inhibitoren von serin proteasen |
| 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 |
| WO2001053260A1 (en) | 2000-01-18 | 2001-07-26 | Novartis Ag | Carboxamides useful as inhibitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion |
| AU2001262185A1 (en) | 2000-04-10 | 2001-10-23 | Novartis Ag | Substituted (hetero)aryl carboxamide derivatives as microsomal triglyceride transfer protein (mtp) and apolipoprotein b (apo b) secretion |
| 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 |
| GB0013378D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Use of therapeutic benzamide derivatives |
| US20020032238A1 (en) | 2000-07-08 | 2002-03-14 | Henning Priepke | Biphenylcarboxylic acid amides, the preparation thereof and the use thereof as medicaments |
| DE10033337A1 (de) | 2000-07-08 | 2002-01-17 | Boehringer Ingelheim Pharma | Biphenylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
| 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 |
| SI1404653T1 (sl) * | 2001-06-28 | 2008-12-31 | Pfizer Prod Inc | S triamidom substituirani indoli, benzofurani in benzotiofeni kot zaviralci mikrosomske prenašalnebeljakovine za trigliceride (MTP) in/ali izločanja apolipoproteina B (APO B) |
| CN1943786A (zh) | 2002-02-28 | 2007-04-11 | 日本烟草产业株式会社 | 酯化合物及其医药用途 |
-
2002
- 2002-05-24 SI SI200230732T patent/SI1404653T1/sl unknown
- 2002-05-24 CN CN2006100941142A patent/CN1880304B/zh not_active Expired - Fee Related
- 2002-05-24 ES ES02780923T patent/ES2307799T3/es not_active Expired - Lifetime
- 2002-05-24 BR BR0210616-7A patent/BR0210616A/pt active Search and Examination
- 2002-05-24 AU AU2002307839A patent/AU2002307839B2/en not_active Ceased
- 2002-05-24 CA CA002451474A patent/CA2451474C/en not_active Expired - Fee Related
- 2002-05-24 JP JP2003508914A patent/JP4139325B2/ja not_active Expired - Lifetime
- 2002-05-24 MX MXPA03011707A patent/MXPA03011707A/es active IP Right Grant
- 2002-05-24 TN TNPCT/IB2002/001876A patent/TNSN03146A1/fr unknown
- 2002-05-24 HR HR20031051A patent/HRP20031051B1/xx not_active IP Right Cessation
- 2002-05-24 KR KR1020057025027A patent/KR100575944B1/ko not_active Expired - Fee Related
- 2002-05-24 EP EP02780923A patent/EP1404653B1/en not_active Expired - Lifetime
- 2002-05-24 PT PT02780923T patent/PT1404653E/pt unknown
- 2002-05-24 CN CN028130219A patent/CN1522246B/zh not_active Expired - Fee Related
- 2002-05-24 NZ NZ528752A patent/NZ528752A/en not_active IP Right Cessation
- 2002-05-24 GE GEAP20027236A patent/GEP20063720B/en unknown
- 2002-05-24 OA OA1200300327A patent/OA12626A/en unknown
- 2002-05-24 AT AT02780923T patent/ATE405548T1/de active
- 2002-05-24 WO PCT/IB2002/001876 patent/WO2003002533A1/en 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 EA EA200301310A patent/EA007008B1/ru not_active IP Right Cessation
- 2002-05-24 CZ CZ20033558A patent/CZ20033558A3/cs unknown
- 2002-05-24 KR KR1020037017167A patent/KR100575919B1/ko not_active Expired - Fee Related
- 2002-05-24 DK DK02780923T patent/DK1404653T3/da active
- 2002-05-24 HU HU0400348A patent/HU229551B1/hu not_active IP Right Cessation
- 2002-05-24 PL PL02367680A patent/PL367680A1/xx unknown
- 2002-05-24 SK SK1610-2003A patent/SK287806B6/sk not_active IP Right Cessation
- 2002-05-24 IL IL15851602A patent/IL158516A0/xx not_active IP Right Cessation
- 2002-05-24 RS YUP-1004/03A patent/RS50712B/sr unknown
- 2002-05-24 DE DE60228447T patent/DE60228447D1/de not_active Expired - Lifetime
- 2002-05-24 GE GE5350A patent/GEP20053720B/en unknown
- 2002-06-20 US US10/177,858 patent/US6720351B2/en not_active Expired - Fee Related
- 2002-06-21 TW TW091113664A patent/TWI313264B/zh not_active IP Right Cessation
- 2002-06-21 TW TW094146513A patent/TW200628447A/zh unknown
- 2002-06-26 MY MYPI20022415A patent/MY129328A/en unknown
- 2002-06-26 AR ARP020102408A patent/AR036158A1/es active IP Right Grant
- 2002-06-27 AP APAP/P/2002/002567A patent/AP1649A/en active
- 2002-06-27 GT GT200200136A patent/GT200200136A/es unknown
- 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 US10/639,855 patent/US6949572B2/en not_active Expired - Fee Related
- 2003-08-13 US US10/639,854 patent/US6979692B2/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 MA MA27457A patent/MA27045A1/fr unknown
- 2003-12-22 BG BG108487A patent/BG108487A/bg 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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20030135A1 (es) | Derivados indol sustituido con triamida como inhibidores de la secrecion de mtp | |
| AR036906A1 (es) | Compuestos de imidazopiridin como moduladores del receptor 5-ht4 | |
| PE20060777A1 (es) | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas | |
| TW200734322A (en) | Indole derivatives exhibiting PGD2 receptor antagonism | |
| PE20010211A1 (es) | Compuestos de tiazol y composiciones farmaceuticas para inhibir las quinasas de proteina | |
| PE20021005A1 (es) | Quinazolinas como inhibidores de mmp-13 | |
| AR030959A1 (es) | Derivados de aminoalcoholes, procedimiento para prepararlos, el uso de los mismos para preparar medicamentos y las composiciones farmaceuticas que las contienen | |
| TW200800938A (en) | Indole carboxylic acid derivatives exhibiting PGD2 receptor antagonism | |
| YU96103A (sh) | Novi derivati indola sa afinitetom za 5-ht6 receptor | |
| PE20070550A1 (es) | Derivados de la 1-amino-ftalazina sustituida afines al receptor mch1 y su preparacion | |
| AR032621A1 (es) | Compuestos derivados de tiofeno, metodo para su preparacion, composicion farmaceutica y uso en la fabricacion de medicamentos | |
| PE20050773A1 (es) | Compuestos de quinolina sustituidos | |
| GB2424882A (en) | Selective kinase inhibitors | |
| SE0104332D0 (sv) | Therapeutic agents | |
| SE0202133D0 (sv) | Novel compounds | |
| AR068413A2 (es) | Derivados 8-amino, metodos de preparacion, composiciones farmaceuticas y su uso en terapia | |
| ATE496620T1 (de) | 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren | |
| TNSN06203A1 (en) | Derivatives of n- (1,5-diphenyl-1h-pyrazol-3-yl) sulphonamide with cb1 receptor affinity | |
| PE20120655A1 (es) | Derivados de triazolopiridina como inhibidores de proteinas cinasas activadas por mitogeno p38 (map) | |
| PE20000945A1 (es) | Compuesto de maleimida disustituida y su uso farmaceutico | |
| MXPA04002495A (es) | Compuestos de imidazopiridin como moduladores del receptor 5-ht4. | |
| PE20020253A1 (es) | Derivados de 3-azabiciclo[3.1.0]hexano como ligandos de receptores opiaceos | |
| AR035110A1 (es) | Compuesto derivado de piperazina, uso del mismo para la preparacion de una composicion farmaceutica, composicion farmaceutica que lo comprende y procedimiento para la preparacion de dicho compuesto | |
| PT902684E (pt) | Derivados hexa-hidro-pirido(4,3-b)indolo utilizados como farmacos antipsicoticos | |
| PE20020444A1 (es) | Antagonistas de receptores de taquiquinina zwitterionica |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |