PE20090897A1 - Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1 - Google Patents
Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1Info
- Publication number
- PE20090897A1 PE20090897A1 PE2008001299A PE2008001299A PE20090897A1 PE 20090897 A1 PE20090897 A1 PE 20090897A1 PE 2008001299 A PE2008001299 A PE 2008001299A PE 2008001299 A PE2008001299 A PE 2008001299A PE 20090897 A1 PE20090897 A1 PE 20090897A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- dgat
- dihydropyrimide
- oxazepin
- perfluoroalkyl
- Prior art date
Links
- 150000001875 compounds Chemical group 0.000 title abstract 4
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 3
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 abstract 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- -1 CYCLOHEXYL Chemical class 0.000 abstract 1
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical class CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/12—Ophthalmic agents for cataracts
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Neurology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
REFERIDO A UN COMPUESTO DERRIVADO DE BICICLOLACTAMA DE FORMULA (1), DONDE R1 ES H, -ALQUILO (C1-C4), -PERFLUOROALQUILO(C1-C4), -PERFLUOROALCOXI(C1-C4) O -ALCOXI(C1-C4); R2 Y R3 SON CADA UNO H, -ALQUILO(C1-C4) O -PERFLUOROALQUILO(C1-C4); O R2 Y R3 JUNTOS CON EL CARBONO AL CUAL ESTAN UNIDOS FORMAN CICLOALQUILO(C3-C6); R4 ES H O -ALQUILO(C1-C4); R5a, R5b, R5c Y R5d SON CADA UNO H, F, -ALQUILO(C1-C4), ENTRE OTROS; Q ES -O- o UN ENLACE; A ES -CICLOALQUILENO(C3-C6), -CICLOALQUENILENO(C3-C6) O FENILENO; Z ES -C(R6a)(R6b) O UN ENLACE, DONDE R6a Y R6b SON CADA UNO -H O -ALQUILO(C1-C4) O R6a Y R6b, TOMADOS JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS, ES UN CICLOALQUILO (C3-C6); R7 ES C(O)R8, CIANO, HIDROXILO, ENTRE OTROS; R8 ES -OR9 O NHR10; R9 ES -H, -ALQUILO(C1-C4) O PERFLUOROALQUILO(C1-C4) Y R10 ES -H, -ALQUILO(C1-C4), TETRAZOLILO O S(O)2CF3. SON COMPUESTOS PREFERIDOS: {TRANS-4-[4-(4-CLORO-5-OXO-7,8-DIHIDROPIRIMIDO[5,4-f][1,4]OXAZEPIN-6-(5H)-IL)FENIL]CICLOHEXIL}ACETATO DE METILO, 2-((1S,4S)-4-(4-((R)-4-CLORO-8-METIL-5-OXO-7,8-DIHIDROPIRIMIDO-[5,4-f][1,4]OXAZEPIN-6(5H)-IL)FENIL)CICLOHEXIL)ACETATO DE METILO, (TRANS-4-{4-[(7S)-4-CLORO-7-METIL-5-OXO-7,8-DIHIDROPIRIMIDO[5,4-f][1,4]OXAZEPIN-6(5H)-IL]FENIL}CICLOHEXIL)ACETATO DE METILO ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN METODO DE PREPARACION. DICHO COMPUESTO TIENE ACTIVIDAD INHIBITORIA SOBRE DGAT-1(DIACILGLICEROL O-ACILTRANSFERASA) Y ES UTIL EN EL TRATAMIENTO DE LA OBESIDAD, DIABETES TIPO 2, ENTRE OTROS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95350707P | 2007-08-02 | 2007-08-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090897A1 true PE20090897A1 (es) | 2009-08-06 |
Family
ID=39926534
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001299A PE20090897A1 (es) | 2007-08-02 | 2008-08-01 | Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1 |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US20090036425A1 (es) |
| EP (1) | EP2185567B1 (es) |
| JP (1) | JP4629808B2 (es) |
| KR (1) | KR20100032443A (es) |
| CN (1) | CN101772504A (es) |
| AP (1) | AP2010005163A0 (es) |
| AR (1) | AR067780A1 (es) |
| AT (1) | ATE502948T1 (es) |
| AU (1) | AU2008281545B2 (es) |
| BR (1) | BRPI0815067A2 (es) |
| CA (1) | CA2695291C (es) |
| CL (1) | CL2008002227A1 (es) |
| CO (1) | CO6251365A2 (es) |
| CR (1) | CR11223A (es) |
| CY (1) | CY1111628T1 (es) |
| DE (1) | DE602008005757D1 (es) |
| DK (1) | DK2185567T3 (es) |
| DO (1) | DOP2010000046A (es) |
| EA (1) | EA201000050A1 (es) |
| EC (1) | ECSP109932A (es) |
| ES (1) | ES2361716T3 (es) |
| HN (1) | HN2008001191A (es) |
| HR (1) | HRP20110335T1 (es) |
| MA (1) | MA31580B1 (es) |
| PA (1) | PA8791601A1 (es) |
| PE (1) | PE20090897A1 (es) |
| PL (1) | PL2185567T3 (es) |
| PT (1) | PT2185567E (es) |
| SI (1) | SI2185567T1 (es) |
| TN (1) | TN2010000053A1 (es) |
| TW (1) | TWI356059B (es) |
| UA (1) | UA94833C2 (es) |
| WO (1) | WO2009016462A2 (es) |
| ZA (1) | ZA201000255B (es) |
Families Citing this family (83)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005315430B2 (en) | 2004-12-14 | 2010-05-27 | Astrazeneca Ab | Oxadiazole derivatives as DGAT inhibitors |
| JP2009520786A (ja) | 2005-12-22 | 2009-05-28 | アストラゼネカ アクチボラグ | Ｄｇａｔ阻害剤として使用するためのピリミド−［４，５−ｂ］−オキサジン |
| EP2402317B1 (en) | 2006-03-31 | 2013-07-03 | Novartis AG | DGAT inhibitor |
| NZ572586A (en) | 2006-05-30 | 2011-03-31 | Astrazeneca Ab | Substituted 5-phenylamino-1,3,4-oxadiazol-2-ylcarbonylamino-4-phenoxy-cyclohexane carboxylic acid as inhibitors of acetyl coenzyme a diacylglycerol acyltransferase |
| CA2655604C (en) | 2006-06-23 | 2016-08-09 | Abbott Laboratories | Cyclopropyl amine derivatives |
| US9108948B2 (en) * | 2006-06-23 | 2015-08-18 | Abbvie Inc. | Cyclopropyl amine derivatives |
| AR066169A1 (es) | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
| TW201038580A (en) * | 2009-02-02 | 2010-11-01 | Pfizer | 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives |
| TW201040174A (en) * | 2009-02-03 | 2010-11-16 | Pfizer | 4-amino-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one derivatives |
| EP2393811A1 (en) * | 2009-02-04 | 2011-12-14 | Pfizer Inc. | 4-amino-7,8-dihydropyrido[4,3-d]pyrimidin-5(6h)-one derivatives |
| EP2805951B1 (en) | 2009-03-20 | 2018-03-14 | Metabasis Therapeutics, Inc. | Inhibitors of diacylglycerol o-acyltransferase 1 (DGAT-1) and uses thereof |
| US9186353B2 (en) | 2009-04-27 | 2015-11-17 | Abbvie Inc. | Treatment of osteoarthritis pain |
| PL2547679T3 (pl) | 2010-03-19 | 2016-02-29 | Pfizer | Pochodne 2,3-dihydro-1H-inden-1-ylo-2,7-diazaspiro[3.5]nonanu i ich zastosowanie jako antagonistów lub odwrotnych agonistów receptora greliny |
| WO2011121350A1 (en) | 2010-04-01 | 2011-10-06 | Astrazeneca Ab | 4 -amino -7,8- dihydropyrimido [5, 4 - f] [1, 4] oxazepin- 5 ( 6h) - one based dgat1 inhibitors |
| WO2012037258A1 (en) | 2010-09-16 | 2012-03-22 | Abbott Laboratories | Processes for preparing 1,2-substituted cyclopropyl derivatives |
| HUE025078T2 (en) | 2010-10-29 | 2016-01-28 | Pfizer | N1 / N2-lactam-acetyl-CoA carboxylase inhibitors |
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| PE20141187A1 (es) | 2011-04-22 | 2014-09-18 | Pfizer | Inhibidores sustituidos de aeitl-coa carboxilasa |
| AU2012253653A1 (en) | 2011-05-10 | 2013-05-02 | Gilead Sciences, Inc. | Fused heterocyclic compounds as sodium channel modulators |
| HRP20161089T1 (hr) * | 2011-05-20 | 2016-10-21 | Glaxosmithkline Intellectual Property (No. 2) Limited | Novi spojevi kao inhibitori diacilglicerol-aciltransferaze |
| NO3175985T3 (es) | 2011-07-01 | 2018-04-28 | ||
| TWI622583B (zh) | 2011-07-01 | 2018-05-01 | 基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| CA2841757A1 (en) | 2011-07-15 | 2013-01-24 | Etzer Darout | Gpr 119 modulators |
| RU2013157388A (ru) | 2011-07-22 | 2015-08-27 | Пфайзер Инк. | Хинолинильные модуляторы глюкагонового рецептора |
| JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 |
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| BR112014031108A2 (pt) | 2012-06-20 | 2017-06-27 | Hoffmann La Roche | compostos de pirazol substituído como antagonistas de lpar |
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| US6995153B2 (en) * | 2002-01-18 | 2006-02-07 | Kyorin Pharmaceutical. Co., Ltd. | Fused bicyclic pyrimidine derivatives |
| RU2342388C2 (ru) * | 2002-11-22 | 2008-12-27 | Джапан Тобакко Инк. | Конденсированные бициклические азотсодержащие гетероциклы, обладающие dgat ингибирующим действием |
| JP2007519605A (ja) * | 2004-01-30 | 2007-07-19 | 日本たばこ産業株式会社 | 食欲抑制薬 |
| JP2006056881A (ja) * | 2004-07-21 | 2006-03-02 | Takeda Chem Ind Ltd | 縮合環化合物 |
| JP2009520786A (ja) * | 2005-12-22 | 2009-05-28 | アストラゼネカ アクチボラグ | Ｄｇａｔ阻害剤として使用するためのピリミド−［４，５−ｂ］−オキサジン |
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