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AR086817A1 - Compuestos inhibidores de la fosfodiesterasa tipo 10a - Google Patents

Compuestos inhibidores de la fosfodiesterasa tipo 10a

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Publication number
AR086817A1
AR086817A1 ARP120102358A ARP120102358A AR086817A1 AR 086817 A1 AR086817 A1 AR 086817A1 AR P120102358 A ARP120102358 A AR P120102358A AR P120102358 A ARP120102358 A AR P120102358A AR 086817 A1 AR086817 A1 AR 086817A1
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Argentina
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alkyl
alkoxy
members
radicals
group
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ARP120102358A
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Inventor
Geneste Herve
Ochse Michael
Drescher Karla
Belh Berthold
Laplanche Loic
Dinges Jurgen
Jakob Clarissa
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Abbott Gmbh & Co Kg
Abbott Lab
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Application filed by Abbott Gmbh & Co Kg, Abbott Lab filed Critical Abbott Gmbh & Co Kg
Publication of AR086817A1 publication Critical patent/AR086817A1/es

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    • 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
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    • A—HUMAN NECESSITIES
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    • 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
    • C07D401/06—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 only aliphatic carbon atoms
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    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07D487/04—Ortho-condensed systems
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    • 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
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compuestos de carboxamida. Composiciones farmacéuticas que los contienen. Su uso en la terapia. Estos compuestos presentan propiedades terapéuticas valiosas y son particularmente apropiados para tratar o controlar diversos trastornos neurológicos y psiquiátricos, para mejorar sus síntomas y para reducir el riesgo de que se desarrollen. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) donde X¹ es N o C-R¹; X² es N o C-R²; X³ es N o C-R³; X⁴ es N o C-R⁴; con la condición de que 0, 1 ó 2 de las porciones X¹, X², X³ o X⁴ es N; A se selecciona entre el grupo que consiste en O, S, S(=O), S(=O)₂, NR⁵ᵃ y CR⁵R⁶; Het se selecciona entre i) hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que no está sustituido o puede tener 1, 2, 3 ó 4 sustituyentes Rˣ idénticos o diferentes, ii) hetarilo bicíclico fusionado con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, benzotienilo o benzofurilo, donde hetarilo, benzotienilo y benzofurilo bicíclico son, en forma independiente entre sí, puede no estar sustituido o puede tener 1, 2, 3 ó 4 sustituyentes Rˣ idénticos o diferentes, y iii) fenilo, que tiene un radical hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que además de hetarilo monocíclico, puede tener 1, 2 ó 3 sustituyentes Rˣ idénticos o diferentes, donde Rˣ se selecciona entre el grupo que consiste en H, halógeno, alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄-alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, OH, hidroxi-alquilo C₁₋₄, O-cicloalquilo C₃₋₆, benciloxi, C(O)O-(alquilo C₁₋₄), O-(alquil C₁₋₄)-CO₂H, N(Rˣ¹)(Rˣ²), C(O)N(Rˣ¹)(Rˣ²), alquil C₁₋₄-N(Rˣ¹)(Rˣ²), -NRˣ³-C(O)-N(Rˣ¹)(Rˣ²), NRˣ³-C(O)O-(alquilo C₁₋₄), -N(Rˣ³)-SO₂-Rˣ⁴, fenilo, CN, -SF₅, -OSF₅, SO₂-Rˣ⁴, SRˣ⁴ y trimetilsililo, donde Rˣ¹, Rˣ², Rˣ³ y Rˣ⁴, se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, fluoroalquilo C₁₋₄ y cicloalquilo C₃₋₆ o Rˣ¹ y Rˣ² forman junto con el átomo de N al cual están unidos un heterociclo con nitrógeno de entre 3 y 7 miembros que puede tener 1, 2 ó 3 heteroátomos diferentes o idénticos adicionales o grupos que contienen heteroátomos seleccionados entre el grupo de O, N, S, SO y SO₂ como miembros del anillo y que puede tener 1, 2, 3, 4, 5 ó 6 sustituyentes seleccionados entre alquilo C₁₋₄; R¹, R⁴ en forma independiente entre sí, se seleccionan entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alquil C₁₋₄sulfanilo, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alquil C₁₋₄sulfanil-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ², NRˣ¹Rˣ²-alcoxi C₁₋₄ y la porción Y-Cyc; R², R³ en forma independiente entre sí, se seleccionan entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ² y la porción Y-Cyc; con la condición de que uno o dos de los radicales R¹, R², R³, R⁴ son una poción Y-Cyc; R⁵, R⁶ se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, OH, halógeno, alquilo C₁₋₄, trimetilsililo, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, y cicloalquilo C₃₋₆ fluorado o los radicales R⁵, R⁶ junto con el átomo de carbono al cual están unidos forman un grupo carbonilo o un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo; R⁵ᵃ se selecciona entre el grupo que consiste en alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, cicloalquilo C₃₋₆ fluorado, fenilo, bencilo, hetarilo de 5 ó 6 miembros con 1, 2 ó 3 heteroátomos seleccionados entre O, S y N como miembros del anillo, y hetarilmetilo de 5 ó 6 miembros con 1, 2 ó 3 heteroátomos seleccionados entre O, S y N como miembros del anillo, donde los anillos en los últimos cuatro radicales mencionados no están sustituidos o tienen 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor, alquilo C₁₋₄, fluoroalquilo C₁₋₄, alcoxi C₁₋₄ y fluoroalcoxi C₁₋₄; R⁷, R⁸, R⁹, R¹⁰ se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, alquilo C₁₋₄, trimetilsililo, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, o los radicales junto con los átomos de carbono a los cuales están unidos forman un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo o los radicales R⁷, R⁸ o los radicales R⁹, R¹⁰ junto con el átomo de carbono al cual están unidos forman un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo; Y es un enlace químico, CH₂, O, O-CH₂, NRʸ, NRʸ-CH₂, NRʸ-S(O)₂, S, S(O), S(O)₂, 1,2-etandiilo, 1,2-etendiilo o 1,2-etindiilo, donde Rʸ se selecciona entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, alquil C₁₋₄carbonilo, alquil C₁₋₄sulfonilo, fluoroalquil C₁₋₄sulfonilo; Cyc es un radical seleccionado entre el grupo que consiste en fenilo, naftilo, radicales monocarbocíclicos saturados o parcialmente insaturados de entre 4 y 8 miembros, radicales bicarbocíclicos saturados o parcialmente insaturados de entre 7 y 10 miembros, radicales heteromonocíclicos saturados o parcialmente insaturados de entre 4 y 8 miembros, radicales heterobicíclicos saturados o parcialmente insaturados de entre 7 y 10 miembros, hetarilo monocíclico de 5 ó 6 miembros, y hetarilo bicíclico de entre 8 y 10 miembros, donde los radicales heteromonocíclicos y heterobicíclicos saturados o parcialmente insaturados tienen 1 2, 3 ó 4 heteroátomos o grupos que contienen heteroátomos como miembros del anillo, que se seleccionan entre O, S, SO, SO₂ y N, y donde el hetarilo monocíclico de 5 ó 6 miembros y el hetarilo bicíclico de entre 8 y 10 miembros tienen 1, 2, 3 ó 4 heteroátomos como miembros del anillo, que se seleccionan entre O, S y N, donde fenilo, naftilo, los radicales mono- y bicarbocíclicos saturados o parcialmente insaturados, los radicales heteromonocíclicos y heterobicíclicos y los radicales heteroaromáticos mono- y bicíclicos no están sustituidos o tienen 1, 2, 3, 4 ó 5 radicales RC¹ o un radical Y-RC² y 0, 1, 2, 3 ó 4 radicales RC¹; donde RC¹ se selecciona entre hidrógeno, halógeno, OH, CN, NO₂, alquilo C₁₋₄, alcoxi C₁₋₄, alquil C₁₋₄sulfanilo, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, ciano-alquilo C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, alquil C₁₋₄sulfonilo, C(O)Rᵃ, Z-C(O)ORᵇ, Z-C(O)NRᶜRᵈ, S(O)₂NRᶜRᵈ y Z-NRᵉRᶠ, donde Rᵃ se selecciona entre el grupo que consiste en alquilo C₁₋₄ y fluoroalquilo C₁₋₄, Rᵇ se
ARP120102358A 2011-06-30 2012-06-29 Compuestos inhibidores de la fosfodiesterasa tipo 10a AR086817A1 (es)

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US (2) US9938269B2 (es)
EP (1) EP2726479A1 (es)
JP (1) JP2014518237A (es)
KR (1) KR20140050028A (es)
CN (1) CN103958504B (es)
AR (1) AR086817A1 (es)
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Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130203756A1 (en) * 2010-10-29 2013-08-08 Jamie L. Bunda Isoindoline pde10 inhibitors
JP6175672B2 (ja) * 2012-04-25 2017-08-09 ラクオリア創薬株式会社 Ｔｔｘ−ｓ遮断薬としてのピロロピリジノン誘導体
DE102012016908A1 (de) 2012-08-17 2014-02-20 Aicuris Gmbh & Co. Kg Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung
US9200005B2 (en) 2013-03-13 2015-12-01 AbbVie Deutschland GmbH & Co. KG Inhibitor compounds of phosphodiesterase type 10A
AU2014230745A1 (en) 2013-03-14 2015-09-03 AbbVie Deutschland GmbH & Co. KG Novel inhibitor compounds of phosphodiesterase type 10A
GB201322334D0 (en) 2013-12-17 2014-01-29 Agency Science Tech & Res Maleimide derivatives as modulators of WNT pathway
MX2016009448A (es) * 2014-01-31 2016-10-13 Hoffmann La Roche (hetero)aril-imidazoles/pirazoles para el tratamiento de trastornos neurologicos.
EA031804B1 (ru) 2014-02-03 2019-02-28 Вайтаи Фармасьютиклз, Инк. Дигидропирролопиридиновые ингибиторы ror-гамма
KR101898364B1 (ko) * 2014-05-22 2018-09-12 에프. 호프만-라 로슈 아게 인돌린-2-온 및 1,3-다이하이드로-피롤로[3,2-c]피리딘-2-온 유도체
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 ＭｎＫ抑制劑及其相關方法
UA118989C2 (uk) 2014-10-14 2019-04-10 Вітае Фармасьютікалс, Інк. Дигідропіролопіридинові інгібітори ror-гамма
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
US9879016B2 (en) 2015-04-17 2018-01-30 Abbvie Inc. Indazolones as modulators of TNF signaling
UY36630A (es) 2015-04-17 2016-11-30 Abbvie Inc Moduladores tricíclicos de la señalización por tnf
TW201706258A (zh) 2015-04-17 2017-02-16 艾伯維有限公司 作為ｔｎｆ信號傳遞調節劑之吲唑酮
EP3331876B1 (en) 2015-08-05 2020-10-07 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
ES2989326T3 (es) 2015-10-21 2024-11-26 Otsuka Pharma Co Ltd Compuestos de benzolactama como inhibidores de la proteína cinasa
EA034440B1 (ru) 2015-10-29 2020-02-07 Эффектор Терапьютикс, Инк. СОЕДИНЕНИЯ ПИРРОЛО-, ПИРАЗОЛО-, ИМИДАЗОПИРИМИДИНА И ПИРИДИНА, КОТОРЫЕ ИНГИБИРУЮТ Mnk1 И Mnk2
CN108602805A (zh) * 2015-10-29 2018-09-28 效应治疗股份有限公司 Mnk1和mnk2的异吲哚啉、氮杂异吲哚啉、二氢茚酮和二氢氮杂茚酮抑制剂
US10000487B2 (en) 2015-11-20 2018-06-19 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers
EP3377482B1 (en) 2015-11-20 2021-05-12 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
KR20180114910A (ko) 2016-02-05 2018-10-19 데날리 테라퓨틱스 인크. 수용체-상호작용 단백질 키나제 1의 억제제
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
PT3552017T (pt) 2016-12-09 2022-05-04 Denali Therapeutics Inc Compostos úteis como inibidores de ripk1
MX2019009653A (es) 2017-02-14 2019-12-19 Effector Therapeutics Inc Inhibidores de mnk sustituidos con piperidina y metodos relacionados con los mismos.
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
WO2018237349A1 (en) * 2017-06-23 2018-12-27 University Of Washington TYPE 1 METHIONYL-ARNT SYNTHASEASE INHIBITORS AND METHODS OF USE
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
US10913739B2 (en) 2017-07-24 2021-02-09 Vitae Pharmaceuticals, LLC (121374) Inhibitors of RORγ
SG11202002032SA (en) 2017-09-22 2020-04-29 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
MX2020003341A (es) 2017-10-18 2020-09-17 Jubilant Epipad LLC Compuestos de imidazo-piridina como inhibidores de pad.
EP3707135A1 (en) 2017-11-06 2020-09-16 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation
HRP20240736T1 (hr) 2017-11-24 2024-11-08 Jubilant Episcribe Llc Heterociklički spojevi kao inhibitori prmt5
CN117720541A (zh) 2018-03-09 2024-03-19 里科瑞尔姆Ip控股有限责任公司 取代的1,2-二氢-3H-吡唑并[3,4-d]嘧啶-3-酮
BR112020018610A2 (pt) 2018-03-13 2020-12-29 Jubilant Prodel LLC Compostos de fórmula i, fórmula ii, fórmula iii, fórmula iv, fórmula v, fórmula vi, ou seus polimorfos, estereoisômeros, tautômeros, profármacos, solvatos e sais farmaceuticamente aceitáveis dos mesmos e uso dos mesmos; processo de preparação; composição farmacêutica; e método para o tratamento e/ou prevenção de várias doenças, que incluem câncer e doenças infecciosas
US20210379061A1 (en) 2018-09-28 2021-12-09 Takeda Pharmaceutical Company Limited Balipodect for treating or preventing autism spectrum disorders
MX2021004763A (es) 2018-10-24 2021-06-08 Effector Therapeutics Inc Formas cristalinas de inhibidores de quinasa de interaccion con map quinasa (mnk).
US11396502B2 (en) 2018-11-13 2022-07-26 Incyte Corporation Substituted heterocyclic derivatives as PI3K inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
CN109608444B (zh) * 2018-11-27 2022-02-11 中国药科大学 含异吲哚啉酮的erk抑制剂及其制备方法与用途
WO2021032935A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors
US11005924B1 (en) 2020-04-01 2021-05-11 Netapp, Inc. Disparity of quality of service (QoS) settings of volumes across a cluster
US11140219B1 (en) 2020-04-07 2021-10-05 Netapp, Inc. Quality of service (QoS) setting recommendations for volumes across a cluster
WO2022115301A1 (en) * 2020-11-24 2022-06-02 Merck Sharp & Dohme Corp. Modified isoindolinones as glucosylceramide synthase inhibitors
US11693563B2 (en) 2021-04-22 2023-07-04 Netapp, Inc. Automated tuning of a quality of service setting for a distributed storage system based on internal monitoring
EP4463229A1 (en) 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide
CN114805052A (zh) * 2022-06-07 2022-07-29 华衍化学(上海)有限公司 一种合成对乙烯基苯甲酸的方法

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1560726A (en) 1976-04-28 1980-02-06 Beecham Group Ltd Isothiazolo-pyridines
JPH02268162A (ja) * 1989-04-10 1990-11-01 Fujisawa Pharmaceut Co Ltd ジフェニルピリジン誘導体
US6339093B1 (en) 1999-10-08 2002-01-15 Hoffmann-La Roche Inc. Isoquinoline derivatives
US20030032579A1 (en) 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
DE10134482A1 (de) 2001-07-16 2003-01-30 Bayer Ag Substituierte Isoindole und ihre Verwendung
US20030166476A1 (en) 2002-01-31 2003-09-04 Winemiller Mark D. Lubricating oil compositions with improved friction properties
WO2004037814A1 (en) 2002-10-25 2004-05-06 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
WO2005012485A2 (en) 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
JP2008501776A (ja) 2004-06-07 2008-01-24 ファイザー・プロダクツ・インク 肥満に関連し、かつメタボリックシンドロームに関連する状態の治療としてのホスホジエステラーゼ１０の阻害
US7244759B2 (en) 2004-07-28 2007-07-17 Celgene Corporation Isoindoline compounds and methods of making and using the same
WO2006028957A1 (en) 2004-09-03 2006-03-16 Memory Pharmaceuticals Corporation 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms
ATE460415T1 (de) 2004-11-29 2010-03-15 Warner Lambert Co Therapeutische pyrazoloä3,4-büpyridine und - indazole
US7521557B2 (en) 2005-05-20 2009-04-21 Bristol-Myers Squibb Company Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
CN101228164A (zh) * 2005-05-20 2008-07-23 布里斯托尔-迈尔斯·斯奎布公司 二肽基肽酶iv的吡咯并吡啶类抑制剂及方法
JP2009504759A (ja) 2005-08-16 2009-02-05 メモリ ファーマセチカル コーポレーション ホスホジエステラーゼ１０阻害剤
NL2000397C2 (nl) 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
WO2007082546A1 (en) 2006-01-20 2007-07-26 H. Lundbeck A/S Use of tofisopam as a pde10a inhibitor
CA2635439A1 (en) 2006-01-27 2007-08-02 Pfizer Products Inc. Aminophthalazine derivative compounds
US20070265270A1 (en) 2006-02-21 2007-11-15 Hitchcock Stephen A Cinnoline derivatives as phosphodiesterase 10 inhibitors
MX2008010668A (es) 2006-02-21 2008-10-01 Amgen Inc Derivados de cinolina como inhibidores de fosfodiesterasa 10.
US20090023756A1 (en) 2006-02-23 2009-01-22 Pfizer Inc Substituted quinazolines as pde10 inhibitors
AU2007221049A1 (en) 2006-02-28 2007-09-07 Amgen Inc. Cinnoline and quinazoline derivates as phosphodiesterase 10 inhibitors
US20070265258A1 (en) 2006-03-06 2007-11-15 Ruiping Liu Quinazoline derivatives as phosphodiesterase 10 inhibitors
CA2644850A1 (en) 2006-03-08 2007-09-13 Amgen Inc. Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors
TW200806625A (en) 2006-05-26 2008-02-01 Astrazeneca Ab Therapeutic compounds
TW200815436A (en) 2006-05-30 2008-04-01 Elbion Ag 4-amino-pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
TW200817400A (en) 2006-05-30 2008-04-16 Elbion Ag Pyrido [3,2-e] pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
WO2008001182A1 (en) 2006-06-26 2008-01-03 Pfizer Products Inc. Tricyclic heteroaryl compounds as pde10 inhibitors
US20080090834A1 (en) 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
PT2057153E (pt) 2006-07-10 2012-11-14 Lundbeck & Co As H Derivados (3-aril-piperazin-1-il) de 6,7- dialcoxiquinazolina, 6,7-dialcoxiftalazina e 6,7-dialcoxiisoquinolina
WO2008020302A2 (en) 2006-08-17 2008-02-21 Pfizer Products Inc. Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors
US20090062277A1 (en) 2007-08-21 2009-03-05 Essa Hu Phosphodiesterase 10 inhibitors
US20090062291A1 (en) 2007-08-22 2009-03-05 Essa Hu Phosphodiesterase 10 inhibitors
US20090054434A1 (en) 2007-08-23 2009-02-26 Amgen Inc. Isoquinolone derivatives as phosphodiesterase 10 inhibitors
TW200918519A (en) 2007-09-19 2009-05-01 Lundbeck & Co As H Cyanoisoquinoline
US20090143392A1 (en) 2007-11-30 2009-06-04 Elbion Gmbh Methods of Treating Obesity and Metabolic Disorders
WO2009070583A1 (en) 2007-11-30 2009-06-04 Wyeth Pyrido[3,2-e]pyrazines, process for preparing the same, and their use as inhibitors of phosphodiesterase 10
WO2009068320A1 (en) 2007-11-30 2009-06-04 Elbion Gmbh Aryl and heteroaryl fused imidazo (1,5-a) pyrazines as inhibitors of phosphodiesterase 10
RU2010126622A (ru) 2007-11-30 2012-01-10 УАЙТ ЭлЭлСи (US) Конденсированные с арилом и гетероарилом имидазо[1, 5-а]пиразины в качестве ингибиторов фосфодиэстеразы 10
CN102307871A (zh) 2008-12-08 2012-01-04 西特里斯药业公司 作为沉默调节蛋白调节剂的异吲哚啉酮和相关的类似物
WO2010138585A1 (en) 2009-05-29 2010-12-02 Merck Sharp & Dohme Corp. Pyrimidinones as pde10 inhibitors
TWI485151B (zh) * 2009-12-17 2015-05-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族苯基咪唑衍生物
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物
US20130203756A1 (en) * 2010-10-29 2013-08-08 Jamie L. Bunda Isoindoline pde10 inhibitors
SI2654750T1 (sl) 2010-12-20 2017-04-26 Pfizer Inc. Nove kondenzirane piridinske spojine kot inhibitorji kazein-kinaz

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