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
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 (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2588162A1 (en) * | 2004-12-14 | 2006-06-22 | Astrazeneca Ab | Oxadiazole derivatives as dgat inhibitors |
EP1966221A1 (en) * | 2005-12-22 | 2008-09-10 | AstraZeneca AB | Pyrimido- [4, 5-]-oxazines for use as dgat inhibitors |
EP2402318A1 (en) | 2006-03-31 | 2012-01-04 | Novartis AG | DGAT inhibitors |
NZ572585A (en) * | 2006-05-30 | 2011-02-25 | Astrazeneca Ab | 1,3,4-Oxadiazole derivatives as DGAT1 inhibitors |
BRPI0712802A2 (pt) * | 2006-05-30 | 2012-10-23 | Astrazeneca Ab | composto, métodos para produzir uma inibição da atividade de dgat1, e para tratar diabete melito e/ou obesidade em um animal de sangue quente, uso de um composto, composição farmacêutica, e, processo para preparar um composto |
NZ573576A (en) * | 2006-06-08 | 2011-01-28 | Astrazeneca Ab | Benzimidazoles and their use for the treatment of diabetes |
ES2558152T3 (es) | 2007-06-08 | 2016-02-02 | Janssen Pharmaceutica, N.V. | Derivados de piperidina/piperazina |
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 |
BRPI0813331A2 (pt) | 2007-06-08 | 2014-12-23 | Janssen Pharmaceutica Nv | Derivados de piperidina/piperazina |
US20090036425A1 (en) | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
JP2010536839A (ja) * | 2007-08-17 | 2010-12-02 | アストラゼネカ アクチボラグ | 化合物979 |
AR066169A1 (es) | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
JP5662803B2 (ja) | 2007-12-20 | 2015-02-04 | アストラゼネカ アクチボラグ | Dgat1阻害剤としてのカルバモイル化合物190 |
PE20140572A1 (es) * | 2008-06-05 | 2014-05-16 | Janssen Pharmaceutica Nv | Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar |
CN102395572A (zh) * | 2008-12-19 | 2012-03-28 | 阿斯利康(瑞典)有限公司 | 1,3,4-噁二唑衍生物及其治疗糖尿病的用途 |
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 |
EP2805951B1 (en) | 2009-03-20 | 2018-03-14 | Metabasis Therapeutics, Inc. | Inhibitors of diacylglycerol o-acyltransferase 1 (DGAT-1) and uses thereof |
MX2011014018A (es) | 2009-06-19 | 2012-02-22 | Astrazeneca Ab | Pirazincarboxamidas como inhibidores de dgati. |
UY33354A (es) * | 2010-04-27 | 2011-12-01 | Takeda Pharmaceutical | Compuesto biciclico como inhibidor acc |
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 |
EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | 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 |
EP2766349B1 (de) | 2011-03-08 | 2016-06-01 | 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 |
US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
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 |
JP2016516708A (ja) * | 2013-03-14 | 2016-06-09 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | ビシクロ[2.2.2]酸のgpr120モジュレーター |
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 |
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US4983731A (en) | 1989-03-17 | 1991-01-08 | Nebraska Department Of Economic Development | Separation and purification of sugar esters |
US5491172A (en) | 1993-05-14 | 1996-02-13 | Warner-Lambert Company | N-acyl sulfamic acid esters (or thioesters), N-acyl sulfonamides, and N-sulfonyl carbamic acid esters (or thioesters) as hypercholesterolemic agents |
IL109431A (en) | 1993-05-14 | 2001-01-11 | Warner Lambert Co | Pharmaceutical compositions containing n-acyl sulfamic acid esters (or thioesters), n-acyl sulfonamides, and n-sulfonyl carbamic acid esters (or thioesters), for regulating plasma cholesterol concentration, and certain such novel compounds |
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GB0021670D0 (en) | 2000-09-04 | 2000-10-18 | Astrazeneca Ab | Chemical compounds |
CA2369967A1 (en) | 2001-02-12 | 2002-08-12 | Joseph Anthony Cornicelli | Methods of treating nuclear factor-kappa b mediated diseases and disorders |
JP4436129B2 (ja) | 2001-08-31 | 2010-03-24 | サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | ジアリールシクロアルキル誘導体、その製造法及びppar−活性剤としてのその使用 |
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FR2840301B1 (fr) | 2002-05-29 | 2007-03-23 | Sanofi Synthelabo | Derives de phenyl-cyclohexyl-propanolamine, leur preparation et leur applicaton en therapeutique |
ATE452879T1 (de) | 2002-07-12 | 2010-01-15 | Sanofi Aventis Deutschland | Heterozyklisch substituierte benzoylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel |
JP4164645B2 (ja) | 2002-08-09 | 2008-10-15 | 株式会社大塚製薬工場 | Dgat阻害剤 |
KR100772297B1 (ko) | 2002-11-22 | 2007-11-02 | 니뽄 다바코 산교 가부시키가이샤 | 융합 비시클릭 질소-함유 헤테로사이클 |
AR044152A1 (es) | 2003-05-09 | 2005-08-24 | Bayer Corp | Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad |
JP2007501801A (ja) | 2003-08-07 | 2007-02-01 | 日本たばこ産業株式会社 | ピロロ[1,2−b]ピリダジン誘導体 |
GB0325192D0 (en) | 2003-10-29 | 2003-12-03 | Astrazeneca Ab | Method of use |
WO2005046670A1 (en) | 2003-11-11 | 2005-05-26 | The Skinny Drink Company | Composition for prevention and treatment of obesity, cardiovascular and coronary artery disease |
JP2005206492A (ja) | 2004-01-21 | 2005-08-04 | Sankyo Co Ltd | スルホンアミド化合物 |
AU2005209115A1 (en) | 2004-01-30 | 2005-08-11 | Japan Tobacco Inc. | Anorectic compounds |
TW200606137A (en) | 2004-07-02 | 2006-02-16 | Sankyo Co | Urea derivatives |
WO2006019020A1 (ja) | 2004-08-16 | 2006-02-23 | Sankyo Company, Limited | 置換されたウレア化合物 |
DE602005025517D1 (de) | 2004-10-15 | 2011-02-03 | Bayer Healthcare Llc | Herstellung und anwendung von biphenyl-4-yl-carbonylaminosäurederivaten zur behandlung von obesitas |
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KR20080015113A (ko) | 2005-06-11 | 2008-02-18 | 아스트라제네카 아베 | Dgat 억제제로서의 옥사디아졸 유도체 |
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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 |
EP1966221A1 (en) * | 2005-12-22 | 2008-09-10 | AstraZeneca AB | Pyrimido- [4, 5-]-oxazines for use as dgat inhibitors |
EP2402318A1 (en) | 2006-03-31 | 2012-01-04 | Novartis AG | DGAT inhibitors |
US20080064717A1 (en) | 2006-05-19 | 2008-03-13 | Rajesh Iyengar | Inhibitors of diacylglycerol O-acyltransferase type 1 enzyme |
US20080015227A1 (en) | 2006-05-19 | 2008-01-17 | Kym Philip R | Inhibitors of diacylglycerol O-acyltransferase type 1 enzyme |
BRPI0712802A2 (pt) | 2006-05-30 | 2012-10-23 | Astrazeneca Ab | composto, métodos para produzir uma inibição da atividade de dgat1, e para tratar diabete melito e/ou obesidade em um animal de sangue quente, uso de um composto, composição farmacêutica, e, processo para preparar um composto |
NZ572585A (en) | 2006-05-30 | 2011-02-25 | Astrazeneca Ab | 1,3,4-Oxadiazole derivatives as DGAT1 inhibitors |
EP2035397A1 (en) | 2006-06-06 | 2009-03-18 | Astra Zeneca AB | Chemical compounds |
NZ573576A (en) | 2006-06-08 | 2011-01-28 | Astrazeneca Ab | Benzimidazoles and their use for the treatment of diabetes |
GB0611506D0 (en) | 2006-06-10 | 2006-07-19 | Astrazeneca Ab | Chemical compounds |
GB0611507D0 (en) | 2006-06-10 | 2006-07-19 | Astrazeneca Ab | Chemical compounds |
GB0611552D0 (en) | 2006-06-12 | 2006-07-19 | Astrazeneca Ab | Chemical compounds |
WO2008011130A2 (en) | 2006-07-21 | 2008-01-24 | Takeda Pharmaceutical Company Limited | Amide compounds |
US7569590B2 (en) | 2006-09-19 | 2009-08-04 | Bristol-Myers Squibb Company | Use of thianecarboxamides as dgat inhibitors |
KR100811100B1 (ko) | 2006-09-27 | 2008-03-06 | 한국생명공학연구원 | 벤즈아졸 유도체를 유효성분으로 함유하는 대사성 질환예방 및 치료용 약학적 조성물 |
KR100795462B1 (ko) | 2006-09-27 | 2008-01-16 | 한국생명공학연구원 | 인돌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 대사성 질환 예방 및 치료용 약학적 조성물 |
MX2009003222A (es) | 2006-10-04 | 2009-04-06 | Hoffmann La Roche | Derivados de 3-piridinocarboxamida y 2-pirazinocarboxamida como agentes elevadores de colesterol de lipoproteina de alta densidad. |
AR063311A1 (es) | 2006-10-18 | 2009-01-21 | Novartis Ag | Compuestos organicos |
JP2010511058A (ja) | 2006-11-29 | 2010-04-08 | アボット・ラボラトリーズ | ジアシルグリセロールo−アシルトランスフェラーゼ1型酵素の阻害薬 |
EP2120911A1 (en) | 2007-02-15 | 2009-11-25 | Prosidion Limited | Amide and urea derivatives for the treatment of metabolic diseases |
GB0707662D0 (en) | 2007-04-20 | 2007-05-30 | Astrazeneca Ab | Chemical compounds |
KR20100019470A (ko) | 2007-04-30 | 2010-02-18 | 아보트 러보러터리즈 | 디아실글리세롤 o-아실트랜스퍼라제 타입 1 효소의 억제제 |
RU2497816C2 (ru) | 2007-04-30 | 2013-11-10 | Эббви Инк. | Ингибиторы фермента диацилглицерин о-ацилтрансферазы типа 1 |
US8058299B2 (en) | 2007-05-22 | 2011-11-15 | Via Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
AU2008253118B2 (en) | 2007-05-22 | 2013-11-21 | Madrigal Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
ES2483898T3 (es) | 2007-06-08 | 2014-08-08 | Janssen Pharmaceutica, N.V. | Derivados de piperidina/piperazina |
BRPI0813331A2 (pt) | 2007-06-08 | 2014-12-23 | Janssen Pharmaceutica Nv | Derivados de piperidina/piperazina |
JO2972B1 (en) | 2007-06-08 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Piperidine / piperazine derivatives |
ES2558152T3 (es) | 2007-06-08 | 2016-02-02 | Janssen Pharmaceutica, N.V. | Derivados de piperidina/piperazina |
WO2009011285A1 (ja) | 2007-07-13 | 2009-01-22 | Taisho Pharmaceutical Co., Ltd. | ヘテロアリールベンゼン化合物 |
US20090036425A1 (en) | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
JP2010536839A (ja) | 2007-08-17 | 2010-12-02 | アストラゼネカ アクチボラグ | 化合物979 |
US20090076275A1 (en) | 2007-09-19 | 2009-03-19 | David Robert Bolin | Diacylglycerol acyltransferase inhibitors |
AR066169A1 (es) | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
WO2009071483A1 (en) | 2007-12-07 | 2009-06-11 | Via Pharmaceuticals, Inc. | 1- (indaz0l-5-yl) -ureas as diacylglycerol acyltransferase inhibitors |
JP5662803B2 (ja) | 2007-12-20 | 2015-02-04 | アストラゼネカ アクチボラグ | Dgat1阻害剤としてのカルバモイル化合物190 |
WO2009112445A1 (en) | 2008-03-10 | 2009-09-17 | Novartis Ag | Method of increasing cellular phosphatidyl choline by dgat1 inhibition |
CN102395572A (zh) | 2008-12-19 | 2012-03-28 | 阿斯利康(瑞典)有限公司 | 1,3,4-噁二唑衍生物及其治疗糖尿病的用途 |
-
2006
- 2006-12-19 EP EP06820571A patent/EP1966221A1/en not_active Withdrawn
- 2006-12-19 US US12/158,252 patent/US7749997B2/en not_active Expired - Fee Related
- 2006-12-19 CN CNA2006800487270A patent/CN101346387A/zh active Pending
- 2006-12-19 WO PCT/GB2006/004761 patent/WO2007071966A1/en active Application Filing
- 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 UY UY30050A patent/UY30050A1/es not_active Application Discontinuation
- 2006-12-21 CL CL200603672A patent/CL2006003672A1/es unknown
-
2010
- 2010-06-08 US US12/796,488 patent/US8017603B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
TW200732341A (en) | 2007-09-01 |
WO2007071966A1 (en) | 2007-06-28 |
US7749997B2 (en) | 2010-07-06 |
UY30050A1 (es) | 2007-07-31 |
US8017603B2 (en) | 2011-09-13 |
US20080306059A1 (en) | 2008-12-11 |
JP2009520786A (ja) | 2009-05-28 |
CN101346387A (zh) | 2009-01-14 |
EP1966221A1 (en) | 2008-09-10 |
CL2006003672A1 (es) | 2008-02-08 |
US20100311737A1 (en) | 2010-12-09 |
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