AR077140A1 - Derivados de pirazina como inhibidores de dgat-1, un proceso para prepararlos y una composicion farmaceutica que los comprende - Google Patents
Derivados de pirazina como inhibidores de dgat-1, un proceso para prepararlos y una composicion farmaceutica que los comprendeInfo
- Publication number
- AR077140A1 AR077140A1 ARP100102161A ARP100102161A AR077140A1 AR 077140 A1 AR077140 A1 AR 077140A1 AR P100102161 A ARP100102161 A AR P100102161A AR P100102161 A ARP100102161 A AR P100102161A AR 077140 A1 AR077140 A1 AR 077140A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- group
- cyano
- independently
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 3
- 229910052794 bromium Inorganic materials 0.000 abstract 3
- 229910052801 chlorine Inorganic materials 0.000 abstract 3
- 239000000460 chlorine Substances 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 239000011737 fluorine Substances 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229940127193 DGAT1 inhibitor Drugs 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 125000004848 alkoxyethyl group Chemical group 0.000 abstract 1
- -1 cyano, hydroxy Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- 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
- A61P3/08—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se describen compuestos inhibidores de DGAT-1 de la formula (1), sales farmacéuticamente aceptables de los mismos, junto con composiciones farmacéuticas, procesos para prepararlos y sus usos en tratar, por ejemplo la obesidad Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptable del mismo, donde cada r es de manera independiente 0 o 1 y cada X1 se selecciona de manera independiente de alquilo (C1-3) lineal, alquenilo (C2-3), alquinilo (C2-3), alcoxi (C1-2), metoximetilo, amino y ciano; cada q es de manera independiente 0 o 1 y cada X2 se selecciona de manera independiente de fluor, cloro, bromo, amino, ciano, alquilo (C1-3), alquenilo (C2-3), alquinilo (C2-3) y alcoxi (C1-2); Y1 se selecciona de fluor, cloro, bromo, ciano, alquilo (C1-3) y alcoxi (C1-2); n es 0, 1 o 2 y cada Y2 se selecciona de manera independiente de fluor, cloro, bromo, ciano, hidroxi, alquilo (C1-3) y alcoxi (C1-2); p es 0, 1 o 2 y cada Y3 es de manera independiente alquilo (C1-3) o cuando p es 2 cada Y3 también se puede ligar para formar un anillo cicloalquilo (C3-5); Z es carboxi o un grupo Q seleccionado de -CONHSO2Me o uno de los anillos del grupo (2), o Z es -CONRbRc donde Rb y Rc se seleccionan de manera independiente de hidrogeno, alquilo (C1-4) y alcoxietilo (C1-4)o Rb y Rc se ligan de manera de formar un anillo morfolino o un anillo heterocíclico (C4-6), y cuando Z es -CONRbRc el grupo alquilo (C1-4) y anillos morfolino o heterocíclico (C4-6) que se pueden formar pueden estar opcionalmente sustituidos en un átomo de carbono disponible con carboxi o un grupo Q; y donde cualquier átomo de carbono en un grupo que contiene alquilo (C1-3) lineal, alquilo (C1-3) o alcoxi (C1-2) que se definio con anterioridad puede estar opcionalmente sustituido con hasta 3 átomos de fluor.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21853909P | 2009-06-19 | 2009-06-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077140A1 true AR077140A1 (es) | 2011-08-03 |
Family
ID=42357808
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102161A AR077140A1 (es) | 2009-06-19 | 2010-06-18 | Derivados de pirazina como inhibidores de dgat-1, un proceso para prepararlos y una composicion farmaceutica que los comprende |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8188092B2 (es) |
| EP (1) | EP2443096A1 (es) |
| JP (1) | JP2012530122A (es) |
| KR (1) | KR20120037939A (es) |
| CN (1) | CN102498103A (es) |
| AR (1) | AR077140A1 (es) |
| AU (1) | AU2010261499A1 (es) |
| BR (1) | BRPI1016109A2 (es) |
| CA (1) | CA2764013A1 (es) |
| MX (1) | MX2011014018A (es) |
| RU (1) | RU2011152517A (es) |
| TW (1) | TW201103895A (es) |
| UY (1) | UY32716A (es) |
| WO (1) | WO2010146395A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090197926A1 (en) * | 2006-06-08 | 2009-08-06 | Alan Martin Birch | Benzimidazoles and their use for the treatment of diabetes |
| 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 |
| EP2684879A1 (en) | 2012-07-09 | 2014-01-15 | Basf Se | Substituted mesoionic compounds for combating animal pests |
| US9550793B2 (en) | 2012-10-03 | 2017-01-24 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| TWI644899B (zh) | 2013-02-04 | 2018-12-21 | 健生藥品公司 | Ｆｌａｐ調節劑 |
| EP3070085B1 (en) * | 2013-02-04 | 2019-01-09 | Janssen Pharmaceutica NV | Flap modulators |
| CN103467392B (zh) * | 2013-10-09 | 2016-08-17 | 重庆工商大学 | 一种多卤代吡嗪甲酰胺衍生物及其盐类、制备方法和用途 |
| CN103880757B (zh) * | 2014-04-15 | 2016-02-24 | 上海毕得医药科技有限公司 | 一种5-羟基嘧啶-2-羧酸的合成方法 |
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| KR100795462B1 (ko) | 2006-09-27 | 2008-01-16 | 한국생명공학연구원 | 인돌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 대사성 질환 예방 및 치료용 약학적 조성물 |
| WO2008040651A1 (en) | 2006-10-04 | 2008-04-10 | F. Hoffmann-La Roche Ag | 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents |
| PE20080888A1 (es) | 2006-10-18 | 2008-08-26 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE LA ACIL-TRANSFERASA DE ACIL-CoA-DIACIL-GLICEROL 1 (DGAT1) |
| WO2008046216A1 (en) | 2006-10-18 | 2008-04-24 | Methylgene, Inc. | Kinase inhibitors and uses thereof |
| EP2081892A4 (en) | 2006-11-17 | 2014-03-05 | Donald F Weaver | COMPOUNDS AND METHOD FOR THE TREATMENT OF PROTEIN DISAPPEARANCE |
| CA2670736A1 (en) | 2006-11-29 | 2008-06-05 | Abbott Laboratories | Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme |
| CN101600437A (zh) | 2006-12-11 | 2009-12-09 | 诺瓦提斯公司 | 预防或治疗心肌缺血的方法 |
| US8242139B2 (en) | 2007-04-30 | 2012-08-14 | Abbott Laboratories | Inhibitors of diacylglycerol O-acyltransferase type 1 enzyme |
| US8058299B2 (en) | 2007-05-22 | 2011-11-15 | Via Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
| CN101827842A (zh) | 2007-08-17 | 2010-09-08 | 阿斯利康(瑞典)有限公司 | 作为dgat抑制剂的噁二唑衍生物 |
| ES2535083T3 (es) * | 2007-12-20 | 2015-05-05 | Astrazeneca Ab | Compuestos de carbamoilo como inhibidores 190 de DGAT1 |
| JP2010132590A (ja) | 2008-12-03 | 2010-06-17 | Astellas Pharma Inc | オキサジアゾール化合物 |
| AU2009329345A1 (en) | 2008-12-19 | 2011-06-30 | Astrazeneca Ab | 1,3,4-oxadiazole derivatives and their uses to treat diabetes |
-
2010
- 2010-06-17 WO PCT/GB2010/051003 patent/WO2010146395A1/en not_active Ceased
- 2010-06-17 BR BRPI1016109A patent/BRPI1016109A2/pt not_active Application Discontinuation
- 2010-06-17 JP JP2012515565A patent/JP2012530122A/ja active Pending
- 2010-06-17 KR KR1020127001363A patent/KR20120037939A/ko not_active Withdrawn
- 2010-06-17 UY UY0001032716A patent/UY32716A/es unknown
- 2010-06-17 EP EP10725494A patent/EP2443096A1/en not_active Withdrawn
- 2010-06-17 TW TW099119725A patent/TW201103895A/zh unknown
- 2010-06-17 AU AU2010261499A patent/AU2010261499A1/en not_active Abandoned
- 2010-06-17 MX MX2011014018A patent/MX2011014018A/es not_active Application Discontinuation
- 2010-06-17 CN CN201080036012XA patent/CN102498103A/zh active Pending
- 2010-06-17 RU RU2011152517/04A patent/RU2011152517A/ru unknown
- 2010-06-17 CA CA2764013A patent/CA2764013A1/en not_active Abandoned
- 2010-06-18 AR ARP100102161A patent/AR077140A1/es unknown
- 2010-06-18 US US12/818,187 patent/US8188092B2/en not_active Expired - Fee Related
-
2012
- 2012-04-25 US US13/455,275 patent/US20120289520A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US8188092B2 (en) | 2012-05-29 |
| UY32716A (es) | 2011-01-31 |
| JP2012530122A (ja) | 2012-11-29 |
| AU2010261499A1 (en) | 2012-01-12 |
| WO2010146395A1 (en) | 2010-12-23 |
| KR20120037939A (ko) | 2012-04-20 |
| BRPI1016109A2 (pt) | 2016-05-17 |
| CA2764013A1 (en) | 2010-12-23 |
| US20120289520A1 (en) | 2012-11-15 |
| CN102498103A (zh) | 2012-06-13 |
| TW201103895A (en) | 2011-02-01 |
| EP2443096A1 (en) | 2012-04-25 |
| MX2011014018A (es) | 2012-02-22 |
| US20100324068A1 (en) | 2010-12-23 |
| RU2011152517A (ru) | 2013-07-27 |
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