AR058562A1 - Derivados de pirimido [4,5 b] (1,4) oxazinas , procedimientos de obtencion y su uso como inhibidores de acetil coa y dgat 1 - Google Patents
Derivados de pirimido [4,5 b] (1,4) oxazinas , procedimientos de obtencion y su uso como inhibidores de acetil coa y dgat 1Info
- Publication number
- AR058562A1 AR058562A1 ARP060105620A ARP060105620A AR058562A1 AR 058562 A1 AR058562 A1 AR 058562A1 AR P060105620 A ARP060105620 A AR P060105620A AR P060105620 A ARP060105620 A AR P060105620A AR 058562 A1 AR058562 A1 AR 058562A1
- Authority
- AR
- Argentina
- Prior art keywords
- dgat
- inhibitors
- pirimido
- acetil
- oxazines
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 102100036869 Diacylglycerol O-acyltransferase 1 Human genes 0.000 title 1
- 108050004099 Diacylglycerol O-acyltransferase 1 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000004893 oxazines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229940127193 DGAT1 inhibitor Drugs 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 1
- 230000003278 mimic effect Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Hematology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Los compuestos de la presente, son inhibidores de DGAT-1 y son por ende utiles en el tratamiento de, por ejemplo, la obesidad. También se dscriben procesos para preparar los compuestos. Reivindicacion 1: Un compuesto de la formula (1) o su sal, donde: R1 se selecciona entre H, metilo y trifluormetilo; R2 es H, Cl o F; el anillo A es bicicloalcanodiilo C7-10 o tricicloalcanodiilo C8-12; R3 es carboxi o un mímico de ácido carboxílico o bioisotero; R4 y R5 son cada uno independientemente H metilo; n es 0 o 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75331205P | 2005-12-22 | 2005-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058562A1 true AR058562A1 (es) | 2008-02-13 |
Family
ID=37806230
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105620A AR058562A1 (es) | 2005-12-22 | 2006-12-19 | Derivados de pirimido [4,5 b] (1,4) oxazinas , procedimientos de obtencion y su uso como inhibidores de acetil coa y dgat 1 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US7749997B2 (es) |
| EP (1) | EP1966221A1 (es) |
| JP (1) | JP2009520786A (es) |
| CN (1) | CN101346387A (es) |
| AR (1) | AR058562A1 (es) |
| CL (1) | CL2006003672A1 (es) |
| TW (1) | TW200732341A (es) |
| UY (1) | UY30050A1 (es) |
| WO (1) | WO2007071966A1 (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008523133A (ja) * | 2004-12-14 | 2008-07-03 | アストラゼネカ アクチボラグ | Dgat阻害剤としてのオキサジアゾール誘導体 |
| US7749997B2 (en) * | 2005-12-22 | 2010-07-06 | Astrazeneca Ab | Pyrimido [4,5-B] -Oxazines for use as DGAT inhibitors |
| EP2301923B1 (en) | 2006-03-31 | 2016-06-08 | Novartis AG | Pyridine derivatives as dgat inhibitors |
| ATE492541T1 (de) * | 2006-05-30 | 2011-01-15 | Astrazeneca Ab | Substituierte 5-phenylamino-1,3,4-oxadiazol-2- ylcarbonylamino-4-phenoxycyclohexancarbonsäuren als inhibitoren von acetylcoenzym-a- diacylglycerolacyltransferase |
| US8003676B2 (en) | 2006-05-30 | 2011-08-23 | Astrazeneca Ab | 1,3,4-oxadiazole derivatives as DGAT1 inhibitors |
| CN101460492A (zh) * | 2006-06-08 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 苯并咪唑及其治疗糖尿病的用途 |
| US8835437B2 (en) | 2007-06-08 | 2014-09-16 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
| AU2008258487B2 (en) | 2007-06-08 | 2012-11-15 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
| ES2483898T3 (es) | 2007-06-08 | 2014-08-08 | Janssen Pharmaceutica, N.V. | Derivados de piperidina/piperazina |
| JO2972B1 (en) | 2007-06-08 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Piperidine / piperazine derivatives |
| US20090036425A1 (en) * | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| MX2010001848A (es) * | 2007-08-17 | 2010-03-10 | Astrazeneca Ab | Derivados de oxadiazol como inhibidores de diacilglicerolaciltrans ferasa (dgat). |
| AR066169A1 (es) | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
| WO2009081195A1 (en) | 2007-12-20 | 2009-07-02 | Astrazeneca Ab | Carbamoyl compounds as dgat1 inhibitors 190 |
| JP5579170B2 (ja) | 2008-06-05 | 2014-08-27 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Dgat阻害剤とppar作動薬を含有する薬剤組み合わせ物 |
| JP2012512860A (ja) * | 2008-12-19 | 2012-06-07 | アストラゼネカ アクチボラグ | 1,3,4−オキサジアゾール誘導体および糖尿病を処置するそれらの使用 |
| WO2010086820A1 (en) * | 2009-02-02 | 2010-08-05 | Pfizer Inc. | 4-amino-5-oxo-7, 8-dihydropyrimido [5,4-f] [1,4] oxazepin-6 (5h) -yl) phenyl derivatives, pharmaceutical compositions and uses thereof |
| EP3366686B9 (en) | 2009-03-20 | 2021-08-04 | Metabasis Therapeutics, Inc. | Inhibitors of diacylglycerol o-acyltransferase 1 (dgat-1) and uses thereof |
| CA2764013A1 (en) | 2009-06-19 | 2010-12-23 | Astrazeneca Ab | Pyrazine carboxamides as inhibitors of dgat1 |
| TW201206911A (en) * | 2010-04-27 | 2012-02-16 | Takeda Pharmaceutical | Bicyclic compound |
| JP5678615B2 (ja) * | 2010-11-30 | 2015-03-04 | Dic株式会社 | フッ素化されたビシクロオクタン構造をもつ化合物およびその液晶組成物 |
| WO2012120056A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8710050B2 (en) | 2011-03-08 | 2014-04-29 | Sanofi | Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012120053A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2013068328A1 (en) * | 2011-11-07 | 2013-05-16 | Intervet International B.V. | Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors |
| US9598390B2 (en) | 2013-03-14 | 2017-03-21 | Bristol-Myers Squibb Company | Bicyclo[2.2.2]acid GPR120 modulators |
| CN112552158B (zh) * | 2020-12-09 | 2023-05-19 | 南京工业大学 | 一种含酮羧酸结构的高吸收铬鞣助剂的制备及应用 |
| CN118852065B (zh) * | 2024-06-24 | 2025-09-12 | 中山大学 | 一种多官能脂环族环氧单体及其制备方法和应用 |
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| JP2007191471A (ja) | 2005-12-21 | 2007-08-02 | Sankyo Co Ltd | ウレア誘導体を含有する医薬 |
| US7749997B2 (en) * | 2005-12-22 | 2010-07-06 | Astrazeneca Ab | Pyrimido [4,5-B] -Oxazines for use as DGAT inhibitors |
| EP2301923B1 (en) | 2006-03-31 | 2016-06-08 | Novartis AG | Pyridine derivatives as dgat inhibitors |
| WO2007137107A2 (en) | 2006-05-19 | 2007-11-29 | Abbott Laboratories | Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme |
| WO2007137103A2 (en) | 2006-05-19 | 2007-11-29 | Abbott Laboratories | Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme |
| ATE492541T1 (de) | 2006-05-30 | 2011-01-15 | Astrazeneca Ab | Substituierte 5-phenylamino-1,3,4-oxadiazol-2- ylcarbonylamino-4-phenoxycyclohexancarbonsäuren als inhibitoren von acetylcoenzym-a- diacylglycerolacyltransferase |
| US8003676B2 (en) * | 2006-05-30 | 2011-08-23 | Astrazeneca Ab | 1,3,4-oxadiazole derivatives as DGAT1 inhibitors |
| JP2009539816A (ja) | 2006-06-06 | 2009-11-19 | アストラゼネカ アクチボラグ | 化学化合物 |
| CN101460492A (zh) | 2006-06-08 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 苯并咪唑及其治疗糖尿病的用途 |
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| GB0707662D0 (en) | 2007-04-20 | 2007-05-30 | Astrazeneca Ab | Chemical compounds |
| NZ580662A (en) | 2007-04-30 | 2012-01-12 | Abbott Lab | Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme used in manufacture of medicament for treatment of diabetes or lipid associated disorders |
| KR20100017508A (ko) | 2007-04-30 | 2010-02-16 | 아보트 러보러터리즈 | 디아실글리세롤 o-아실트랜스퍼라제 타입 1 효소의 억제제 |
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| JO2972B1 (en) | 2007-06-08 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Piperidine / piperazine derivatives |
| US8835437B2 (en) | 2007-06-08 | 2014-09-16 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
| ES2483898T3 (es) | 2007-06-08 | 2014-08-08 | Janssen Pharmaceutica, N.V. | Derivados de piperidina/piperazina |
| AU2008258487B2 (en) | 2007-06-08 | 2012-11-15 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
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| WO2009071483A1 (en) | 2007-12-07 | 2009-06-11 | Via Pharmaceuticals, Inc. | 1- (indaz0l-5-yl) -ureas as diacylglycerol acyltransferase inhibitors |
| WO2009081195A1 (en) | 2007-12-20 | 2009-07-02 | Astrazeneca Ab | Carbamoyl compounds as dgat1 inhibitors 190 |
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| JP2012512860A (ja) * | 2008-12-19 | 2012-06-07 | アストラゼネカ アクチボラグ | 1,3,4−オキサジアゾール誘導体および糖尿病を処置するそれらの使用 |
-
2006
- 2006-12-19 US US12/158,252 patent/US7749997B2/en not_active Expired - Fee Related
- 2006-12-19 EP EP06820571A patent/EP1966221A1/en not_active Withdrawn
- 2006-12-19 WO PCT/GB2006/004761 patent/WO2007071966A1/en not_active Ceased
- 2006-12-19 CN CNA2006800487270A patent/CN101346387A/zh active Pending
- 2006-12-19 AR ARP060105620A patent/AR058562A1/es not_active Application Discontinuation
- 2006-12-19 JP JP2008546591A patent/JP2009520786A/ja active Pending
- 2006-12-20 TW TW095147994A patent/TW200732341A/zh unknown
- 2006-12-21 CL CL200603672A patent/CL2006003672A1/es unknown
- 2006-12-21 UY UY30050A patent/UY30050A1/es not_active Application Discontinuation
-
2010
- 2010-06-08 US US12/796,488 patent/US8017603B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN101346387A (zh) | 2009-01-14 |
| TW200732341A (en) | 2007-09-01 |
| UY30050A1 (es) | 2007-07-31 |
| US8017603B2 (en) | 2011-09-13 |
| CL2006003672A1 (es) | 2008-02-08 |
| JP2009520786A (ja) | 2009-05-28 |
| US20080306059A1 (en) | 2008-12-11 |
| US7749997B2 (en) | 2010-07-06 |
| EP1966221A1 (en) | 2008-09-10 |
| WO2007071966A1 (en) | 2007-06-28 |
| US20100311737A1 (en) | 2010-12-09 |
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