ECSP10010274A - Compuestos de carbamoílo como inhibidores de dgat1 190 - Google Patents
Compuestos de carbamoílo como inhibidores de dgat1 190Info
- Publication number
- ECSP10010274A ECSP10010274A EC2010010274A ECSP10010274A ECSP10010274A EC SP10010274 A ECSP10010274 A EC SP10010274A EC 2010010274 A EC2010010274 A EC 2010010274A EC SP10010274 A ECSP10010274 A EC SP10010274A EC SP10010274 A ECSP10010274 A EC SP10010274A
- Authority
- EC
- Ecuador
- Prior art keywords
- ring
- phenylene
- optionally substituted
- direct link
- compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 102100036869 Diacylglycerol O-acyltransferase 1 Human genes 0.000 title 1
- 101000927974 Homo sapiens Diacylglycerol O-acyltransferase 1 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 abstract 2
- -1 2,6-pyrazindiyl Chemical group 0.000 abstract 2
- 150000001924 cycloalkanes Chemical class 0.000 abstract 2
- 229940127193 DGAT1 inhibitor Drugs 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D401/10—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 carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Se describen compuestos inhibidores de DGAT-1 de la fórmula (I), sales aceptables para uso farmacéutico y prodrogas de los mismos, junto con composiciones farmacéuticas, procesos para elaborarlos y su uso en el tratamiento de, por ejemplo, la obesidad en donde, por ejemplo, el Anillo A es 2,6-pirazindiilo opcionalmente sustituido; X es =O; el Anillo B es 1,4-fenileno opcionalmente sustituido; Y1 es un enlace directo o -O-; Y2 es -(CH2)r- en donde r es 2 ó 3; n es 0 o n es 1 cuando Y1 es un enlace directo entre el Anillo B y el Anillo C y cuando el Anillo B es 1,4-fenileno y el Anillo C es (4-6C)cicloalcano; el Anillo C es (4-6C)cicloalcano, (7-10C)bicicloalcano, (8-12C)tricicloalcano, fenileno o piridindiilo opcionalmente sustituido; L es un enlace directo o -O-; p es 0, 1 ó 2 y cuando p es 1 RA1 y RA2 son, cada uno de manera independiente, hidrógeno o (1-4C)alquilo; Z es carboxi o un mimético o un bioisóstero del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1539707P | 2007-12-20 | 2007-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP10010274A true ECSP10010274A (es) | 2010-07-30 |
Family
ID=40427160
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2010010274A ECSP10010274A (es) | 2007-12-20 | 2010-06-18 | Compuestos de carbamoílo como inhibidores de dgat1 190 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US7994179B2 (es) |
| EP (1) | EP2234978B1 (es) |
| JP (1) | JP5662803B2 (es) |
| KR (1) | KR20100099738A (es) |
| CN (1) | CN101932562B (es) |
| AR (1) | AR069802A1 (es) |
| AU (1) | AU2008339570B2 (es) |
| BR (1) | BRPI0821274A2 (es) |
| CA (1) | CA2707660A1 (es) |
| CL (1) | CL2008003847A1 (es) |
| CO (1) | CO6290685A2 (es) |
| CR (1) | CR11518A (es) |
| DO (1) | DOP2010000192A (es) |
| EA (1) | EA201001015A1 (es) |
| EC (1) | ECSP10010274A (es) |
| ES (1) | ES2535083T3 (es) |
| IL (1) | IL206045A0 (es) |
| NI (1) | NI201000108A (es) |
| NZ (1) | NZ586104A (es) |
| PE (1) | PE20091682A1 (es) |
| TW (1) | TW200932235A (es) |
| WO (1) | WO2009081195A1 (es) |
| ZA (1) | ZA201003979B (es) |
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| 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 |
| SG173312A1 (en) | 2006-06-23 | 2011-08-29 | Abbott Lab | Cyclopropyl amine derivatives as histamin h3 receptor modulators |
| US9108948B2 (en) | 2006-06-23 | 2015-08-18 | Abbvie Inc. | Cyclopropyl amine derivatives |
| 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 |
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-
2008
- 2008-12-18 WO PCT/GB2008/051199 patent/WO2009081195A1/en not_active Ceased
- 2008-12-18 PE PE2008002123A patent/PE20091682A1/es not_active Application Discontinuation
- 2008-12-18 CN CN2008801259853A patent/CN101932562B/zh not_active Expired - Fee Related
- 2008-12-18 NZ NZ586104A patent/NZ586104A/en not_active IP Right Cessation
- 2008-12-18 AR ARP080105523A patent/AR069802A1/es not_active Application Discontinuation
- 2008-12-18 EP EP08865783.8A patent/EP2234978B1/en active Active
- 2008-12-18 AU AU2008339570A patent/AU2008339570B2/en not_active Expired - Fee Related
- 2008-12-18 BR BRPI0821274A patent/BRPI0821274A2/pt not_active IP Right Cessation
- 2008-12-18 EA EA201001015A patent/EA201001015A1/ru unknown
- 2008-12-18 CA CA2707660A patent/CA2707660A1/en not_active Abandoned
- 2008-12-18 TW TW097149460A patent/TW200932235A/zh unknown
- 2008-12-18 KR KR1020107016252A patent/KR20100099738A/ko not_active Withdrawn
- 2008-12-18 JP JP2010538918A patent/JP5662803B2/ja not_active Expired - Fee Related
- 2008-12-18 ES ES08865783.8T patent/ES2535083T3/es active Active
- 2008-12-19 US US12/339,349 patent/US7994179B2/en not_active Expired - Fee Related
- 2008-12-19 CL CL2008003847A patent/CL2008003847A1/es unknown
-
2010
- 2010-05-27 IL IL206045A patent/IL206045A0/en unknown
- 2010-06-03 ZA ZA2010/03979A patent/ZA201003979B/en unknown
- 2010-06-18 NI NI201000108A patent/NI201000108A/es unknown
- 2010-06-18 CR CR11518A patent/CR11518A/es not_active Application Discontinuation
- 2010-06-18 EC EC2010010274A patent/ECSP10010274A/es unknown
- 2010-06-18 DO DO2010000192A patent/DOP2010000192A/es unknown
- 2010-06-21 CO CO10074457A patent/CO6290685A2/es not_active Application Discontinuation
-
2011
- 2011-05-05 US US13/101,926 patent/US20120108602A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN101932562A (zh) | 2010-12-29 |
| ZA201003979B (en) | 2011-11-30 |
| EP2234978A1 (en) | 2010-10-06 |
| CN101932562B (zh) | 2013-06-12 |
| DOP2010000192A (es) | 2010-07-15 |
| WO2009081195A1 (en) | 2009-07-02 |
| CA2707660A1 (en) | 2009-07-02 |
| JP5662803B2 (ja) | 2015-02-04 |
| AU2008339570A1 (en) | 2009-07-02 |
| JP2011507823A (ja) | 2011-03-10 |
| EA201001015A1 (ru) | 2011-02-28 |
| CL2008003847A1 (es) | 2009-11-27 |
| AR069802A1 (es) | 2010-02-17 |
| IL206045A0 (en) | 2010-11-30 |
| ES2535083T3 (es) | 2015-05-05 |
| EP2234978B1 (en) | 2015-02-25 |
| NI201000108A (es) | 2012-05-14 |
| US7994179B2 (en) | 2011-08-09 |
| US20120108602A1 (en) | 2012-05-03 |
| NZ586104A (en) | 2012-02-24 |
| TW200932235A (en) | 2009-08-01 |
| US20090298853A1 (en) | 2009-12-03 |
| BRPI0821274A2 (pt) | 2017-06-13 |
| CO6290685A2 (es) | 2011-06-20 |
| KR20100099738A (ko) | 2010-09-13 |
| AU2008339570B2 (en) | 2012-04-12 |
| CR11518A (es) | 2010-07-15 |
| PE20091682A1 (es) | 2009-12-04 |
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