AR076024A1 - Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos - Google Patents
Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismosInfo
- Publication number
- AR076024A1 AR076024A1 ARP100101073A ARP100101073A AR076024A1 AR 076024 A1 AR076024 A1 AR 076024A1 AR P100101073 A ARP100101073 A AR P100101073A AR P100101073 A ARP100101073 A AR P100101073A AR 076024 A1 AR076024 A1 AR 076024A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- heteroaryl
- cycloalkyl
- alkylene
- 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
- C07D498/08—Bridged 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
- A61P3/08—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
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/08—Bridged systems
Abstract
La presente se refiere a derivados de heterociclos bicíclicos puenteados, a composiciones que comprenden un derivado de heterociclos bicíclicos puenteados, y a métodos que utilizan los derivados de heterociclos bicíclicos puenteados para tratar o prevenir la obesidad, la diabetes, un trastorno metabolico, una enfermedad cardiovascular o un trastorno relacionado con la actividad de un GPCR en un paciente. Reivindicacion 1: Un compuesto que tiene la formula (1) o una sal aceptable para uso farmacéutico, solvato, éster, prodroga o estereoisomero del mismo, donde A es piridilo o pirimidinilo, donde dicho piridilo y dicho pirimidinilo pueden estar opcionalmente sustituidos con hasta 2 grupos, que pueden ser iguales o diferentes, y se seleccionan de alquilo, cicloalquilo, halo y -O-alquilo; B es fenilo o heteroarilo de 6 miembros, donde dicho fenilo o dicho heteroarilo de 6 miembros puede estar opcionalmente sustituido con hasta 3 grupos, que pueden ser iguales o diferentes, y se seleccionan de alquilo, heterocicloalquilo, heteroarilo, halo, -CN, -S(O)2alquilo y -S(O)2cicloalquilo, donde dichos grupos sustituyentes de heterocicloalquilo o heteroarilo pueden estar no sustituidos o sustituidos opcionalmente con alquilo, y donde un grupo anular -CH2- sobre dicho grupo sustituyente de heterocicloalquilo puede estar opcionalmente reemplazado con un grupo -C(O)-; W es un enlace, -C(O)-, -C(O)NH-, -C(O)-O-, -C(O)-S- o -S(O)2-; X es -O-(alquilen)- o -NH-; Y es -O- o -NH-; Z es un enlace, -C(O)-,-C(R1)2-, -O-, -S(O)2- o -N(R4)-, cada aparicion de R1 es independientemente H o -OH; donde dos grupos R1, junto con los átomos de carbono a los que están unidos, pueden unirse para formar un grupo cicloalquilo de 3 a 6 miembros o un grupo heterocicloalquilo de 3 a 6 miembros; R3 es alquilo, -alquilen-arilo, -alquilen-cicloalquilo, haloalquilo, heteroarilo, -alquilen-O-alquilo, donde dicho grupo haloalquilo puede estar opcionalmente sustituido con un grupo -OH; y donde dicho grupo heteroarilo puede estar opcionalmente sustituido con un grupo seleccionado de alquilo, halo, -O-alquilo y cicloalquilo; y donde el resto cicloalquilo de dicho grupo -alquilen-cicloalquilo puede estar opcionalmente sustituido con alquilo, -O-alquilo o -alquilen-O-alquilo; R4 es H, haloalquilo, arilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo o heteroarilo; n es un numero entero que oscila de 1 a 4. p es 0 o 1; q es 0 o 1; r es 0 o 1; s es 0 o 1; t es 0 o 1; y u es 0 o 1.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16642209P | 2009-04-03 | 2009-04-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR076024A1 true AR076024A1 (es) | 2011-05-11 |
Family
ID=42262311
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100101073A AR076024A1 (es) | 2009-04-03 | 2010-03-31 | Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos |
Country Status (5)
Country | Link |
---|---|
US (1) | US20120040975A1 (es) |
EP (1) | EP2414334A1 (es) |
AR (1) | AR076024A1 (es) |
TW (1) | TW201102393A (es) |
WO (1) | WO2010114958A1 (es) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8815876B2 (en) | 2008-07-16 | 2014-08-26 | Merck Sharp & Dohme Corp. | Bicyclic heterocycle derivatives and methods of use thereof |
EP2318404B1 (en) | 2008-07-16 | 2013-08-21 | Merck Sharp & Dohme Corp. | Bicyclic heterocycle derivatives and use thereof as gpr119 modulators |
US8410122B2 (en) | 2008-12-23 | 2013-04-02 | Merck Sharp & Dohme Corp. | Bicyclic heterocycle derivatives and methods of use thereof |
JP2012526096A (ja) * | 2009-05-08 | 2012-10-25 | ファイザー・インク | Gpr119調節因子 |
KR20120046188A (ko) | 2009-06-24 | 2012-05-09 | 뉴로크린 바이오사이언시즈 인코퍼레이티드 | 신규 화합물, 약제학적 조성물 및 이에 관련된 방법 |
TW201113269A (en) | 2009-06-24 | 2011-04-16 | Boehringer Ingelheim Int | New compounds, pharmaceutical composition and methods relating thereto |
US8609676B2 (en) * | 2009-08-04 | 2013-12-17 | Merck Sharp & Dohme, Corp. | 4, 5, 6-trisubstituted pyrimidine derivatives as factor IXa inhibitors |
EP2503891B1 (en) | 2009-11-23 | 2016-08-03 | Merck Sharp & Dohme Corp. | Pyrimidine ether derivatives and methods of use thereof |
EP2503887B1 (en) | 2009-11-24 | 2016-01-06 | Merck Sharp & Dohme Corp. | Substituted biaryl derivatives and methods of use thereof |
EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | Boehringer Ingelheim International GmbH | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
AU2012267556B9 (en) | 2011-06-09 | 2017-05-11 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of GPR-119 |
TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
CA2960791C (en) | 2014-09-11 | 2023-03-14 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
AR110122A1 (es) | 2016-11-08 | 2019-02-27 | Hoffmann La Roche | Fenoxitriazoles |
US10865194B2 (en) | 2017-11-03 | 2020-12-15 | Fondazione Istituto Italiano Di Tecnologia | Therapeutically active bicyclic-sulphonamides and pharmaceutical compositions |
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IL68769A (en) | 1983-05-23 | 1986-02-28 | Hadassah Med Org | Pharmaceutical compositions containing insulin for oral administration |
US4849405A (en) | 1984-05-09 | 1989-07-18 | Synthetic Blood Corporation | Oral insulin and a method of making the same |
WO1985005029A1 (en) | 1984-05-09 | 1985-11-21 | Medaphore Inc. | Oral insulin and a method of making the same |
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FR2802817B1 (fr) | 1999-12-23 | 2002-10-11 | Centre Nat Rech Scient | Nouveaux inhibiteurs de glycosidases et leurs applications pharmacologiques, notamment pour traiter le diabete |
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JP2002185490A (ja) | 2000-12-19 | 2002-06-28 | Denso Corp | 通信システム及び端末装置 |
GB0212048D0 (en) | 2002-05-24 | 2002-07-03 | Merck Sharp & Dohme | Therapeutic agents |
ATE374766T1 (de) | 2003-01-14 | 2007-10-15 | Arena Pharm Inc | 1,2,3-trisubstituierte aryl- und heteroarylderivate als modulatoren des metabolismus zur vorbeugung und behandlung von metabolismus-bedingten krankheiten wie diabetes oder hyperglykämie |
ES2316964T3 (es) | 2003-02-24 | 2009-04-16 | Arena Pharmaceuticals, Inc. | Fenil-y piridilpipereidinia-derivados como moduladores del metabolismo de la glucosa. |
AR045047A1 (es) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
CA2608405A1 (en) | 2005-05-17 | 2006-11-23 | Schering Corporation | Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia |
US7750015B2 (en) | 2005-05-17 | 2010-07-06 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
DE602006006461D1 (de) | 2005-09-16 | 2009-06-04 | Arena Pharm Inc | Stoffwechselmodulatoren und behandlung damit verbundener erkrankungen |
US7605170B2 (en) * | 2005-12-01 | 2009-10-20 | N.V. Organon | 8-azabicyclo[3.2.1]octane derivatives |
CN101506175A (zh) * | 2006-06-15 | 2009-08-12 | 贝林格尔·英格海姆国际有限公司 | 作为蛋白激酶C-α抑制剂的2-苯氨基-4-(杂环基)氨基-嘧啶 |
JP5415957B2 (ja) * | 2006-12-13 | 2014-02-12 | エフ.ホフマン−ラ ロシュ アーゲー | 非ヌクレオシド逆転写酵素阻害剤としての2−(ピペリジン−4−イル)−4−フェノキシ−又はフェニルアミノ−ピリミジン誘導体 |
GB0719644D0 (en) * | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
AU2008317057B8 (en) * | 2007-10-22 | 2014-02-13 | Merck Sharp & Dohme Corp. | Bicyclic Heterocycle Derivatives and their use as modulators of the activity of GPR119 |
-
2010
- 2010-03-31 AR ARP100101073A patent/AR076024A1/es not_active Application Discontinuation
- 2010-04-01 WO PCT/US2010/029555 patent/WO2010114958A1/en active Application Filing
- 2010-04-01 US US13/260,950 patent/US20120040975A1/en not_active Abandoned
- 2010-04-01 EP EP10713072A patent/EP2414334A1/en not_active Withdrawn
- 2010-04-02 TW TW099110441A patent/TW201102393A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
EP2414334A1 (en) | 2012-02-08 |
US20120040975A1 (en) | 2012-02-16 |
TW201102393A (en) | 2011-01-16 |
WO2010114958A1 (en) | 2010-10-07 |
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FA | Abandonment or withdrawal |