TW201206902A - Unsaturated nitrogen heterocyclic compounds useful as PDE10 inhibitors - Google Patents

Unsaturated nitrogen heterocyclic compounds useful as PDE10 inhibitors Download PDF

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Publication number
TW201206902A
TW201206902A TW100116952A TW100116952A TW201206902A TW 201206902 A TW201206902 A TW 201206902A TW 100116952 A TW100116952 A TW 100116952A TW 100116952 A TW100116952 A TW 100116952A TW 201206902 A TW201206902 A TW 201206902A
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Taiwan
Prior art keywords
azetidin
alkyl
phenyl
pyrazine
doc
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TW100116952A
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English (en)
Chinese (zh)
Inventor
Jennifer R Allen
Essa Hu
Robert M Rzasa
Wenge Zhong
Qingyian Liu
Michael J Frohn
Jian J Chen
Shannon Rumfelt
Alexander J Pickrell
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Amgen Inc
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Application filed by Amgen Inc filed Critical Amgen Inc
Publication of TW201206902A publication Critical patent/TW201206902A/zh

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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
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    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
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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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    • 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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    • 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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    • 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
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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TW100116952A 2010-05-13 2011-05-13 Unsaturated nitrogen heterocyclic compounds useful as PDE10 inhibitors TW201206902A (en)

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US33452510P 2010-05-13 2010-05-13

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US (3) US8957073B2 (enExample)
EP (1) EP2569300A1 (enExample)
JP (1) JP5702855B2 (enExample)
KR (1) KR101564806B1 (enExample)
CN (1) CN103221404B (enExample)
AR (1) AR081627A1 (enExample)
AU (1) AU2011253057B2 (enExample)
BR (1) BR112012029026A2 (enExample)
CA (1) CA2798490A1 (enExample)
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EA (1) EA201291236A1 (enExample)
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MA (1) MA34300B1 (enExample)
MX (1) MX2012013130A (enExample)
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PE (1) PE20130576A1 (enExample)
PH (1) PH12012502212A1 (enExample)
SG (1) SG185515A1 (enExample)
TN (1) TN2012000530A1 (enExample)
TW (1) TW201206902A (enExample)
UA (1) UA109438C2 (enExample)
UY (1) UY33382A (enExample)
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ZA (1) ZA201208510B (enExample)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA34300B1 (fr) * 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
JP2013526546A (ja) 2010-05-13 2013-06-24 アムジエン・インコーポレーテツド Ｐｄｅ１０阻害剤としてのヘテロアリ−ルオキシヘテロシクリル化合物
AU2011253058A1 (en) 2010-05-13 2012-12-06 Amgen Inc. Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
US8946230B2 (en) 2010-05-13 2015-02-03 Amgen Inc. Aryl- and heteroaryl- nitrogen-heterocyclic compounds as PDE10 inhibitors
MX2013009575A (es) 2011-02-18 2014-10-14 Exonhit Therapeutics Sa Derivados de 6, 7-dialcoxi-3-isoquinolinol sustituidos como inhibidores de fosfodiesterasa 10 (pdei0a).
SG10201604682VA (en) 2011-06-10 2016-07-28 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
US8623860B2 (en) * 2011-12-30 2014-01-07 Boehringer Ingelheim International Gmbh Azetidine derivatives, pharmaceutical compositions and uses thereof
TW201348231A (zh) * 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
CA2872989A1 (en) * 2012-05-09 2013-11-14 Zoetis Llc Azetidine derivatives as antiparasitic agents
UY34858A (es) * 2012-06-14 2013-11-29 Amgen Inc Compuestos de azetidina y piperidina útiles como inhibidores de pde10
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
EP3763367A1 (en) 2012-12-06 2021-01-13 Celgene Quanticel Research, Inc. Pyridine-pyrazole derivatives as histone demethylase inhibitors
JP2016507538A (ja) * 2013-02-07 2016-03-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 置換キノキサリン誘導体およびｍＧｌｕＲ４の正のアロステリックモジュレーターとしてのそれらの使用
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
PE20161573A1 (es) 2014-02-13 2017-01-19 Incyte Corp Ciclopropilamina como inhibidor de la lsd1
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
TWI664164B (zh) 2014-02-13 2019-07-01 美商英塞特控股公司 作為ｌｓｄ１抑制劑之環丙胺
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
JP6484640B2 (ja) * 2014-02-14 2019-03-13 武田薬品工業株式会社 Ｇｐｒ６のピラジンモジュレーター
CN104016909B (zh) * 2014-04-03 2016-04-20 定陶县友帮化工有限公司 一种2-氨基-3-溴-5-氯吡啶的合成方法
CN104016911A (zh) * 2014-04-03 2014-09-03 定陶县友帮化工有限公司 一种2-氨基-3,5-二溴吡啶的合成方法
CA2949511A1 (en) * 2014-05-19 2015-11-26 Merial, Inc. Anthelmintic compounds
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
BR112017003745A2 (pt) 2014-08-29 2017-12-05 Tes Pharma S R L inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico
US9855249B2 (en) 2014-10-02 2018-01-02 Flatley Discovery Lab, Llc Isoxazole compounds and methods for the treatment of cystic fibrosis
MY191796A (en) 2015-04-03 2022-07-15 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
US20200321533A1 (en) * 2016-05-24 2020-10-08 President And Fellows Of Harvard College Compounds for organic light emitting diode materials
CA3026149A1 (en) 2016-06-02 2017-12-07 Cadent Therapeutics, Inc. Potassium channel modulators
EA037318B1 (ru) * 2016-12-16 2021-03-11 Пфайзер Инк. Агонисты рецептора glp-1 и их применение
BR112019014814B1 (pt) 2017-01-23 2024-03-12 Novartis Ag Compostos, composições farmacêuticas dos mesmos e seus usos no tratamento de doenças associadas à disfunção de canais iônicos de potássio
CN106957300A (zh) * 2017-04-12 2017-07-18 苏州汉德创宏生化科技有限公司 抗肿瘤杂环药物中间体2‑(3‑氮杂环丁基）吡啶二盐酸盐的合成方法
US11306059B2 (en) 2017-10-25 2022-04-19 University Of South Florida Drug-induced activation of the Reelin signaling system
HRP20220991T1 (hr) 2017-10-27 2022-11-11 Boehringer Ingelheim International Gmbh Derivati piridina i njihova terapeutska uporaba kao inhibitora trpc6
WO2019129025A1 (zh) * 2017-12-26 2019-07-04 迈第康(上海)生物医药科技有限公司 四氢吡咯类化合物、其制备方法、药物组合物及用途
IL277071B2 (en) 2018-03-08 2024-07-01 Incyte Corp AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
US10934279B2 (en) 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
ES2943510T3 (es) * 2018-06-15 2023-06-13 Pfizer Agonistas del receptor GLP-1 y usos del mismo
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US20210395228A1 (en) 2018-10-02 2021-12-23 Syngenta Participations Ag Pesticidally active benzene- and azine-amide compounds
CA3116339A1 (en) 2018-10-22 2020-04-30 Cadent Therapeutics, Inc. Crystalline forms of potassium channel modulators
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
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
EA202191432A1 (ru) 2018-11-22 2021-10-14 Цилу Регор Терапьютикс Инк. Агонисты glp-1r и их применения
JP7157821B2 (ja) 2018-11-26 2022-10-20 京セラ株式会社 ガスノズルおよびガスノズルの製造方法ならびにプラズマ処理装置
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
TWI853009B (zh) 2019-03-29 2024-08-21 瑞士商先正達農作物保護公司 殺有害生物活性之二-醯胺化合物
PE20220171A1 (es) 2019-04-05 2022-01-28 Syngenta Crop Protection Ag Compuestos de diazina-amida activos como pesticidas
US20220169629A1 (en) 2019-04-11 2022-06-02 Syngenta Crop Protection Ag Pesticidally active diazine-amide compounds
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
WO2020207474A1 (en) 2019-04-12 2020-10-15 Qilu Regor Therapeutics Inc. Glp-1r agonists and uses thereof
CA3140972C (en) * 2019-05-20 2024-06-18 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases
CN114269732A (zh) 2019-08-23 2022-04-01 先正达农作物保护股份公司 杀有害生物活性的吡嗪-酰胺化合物
JP7534390B2 (ja) * 2019-09-12 2024-08-14 ディスアーム セラピューティクス， インコーポレイテッド Ｓａｒｍ１の阻害剤
IL292943A (en) * 2019-11-15 2022-07-01 Ildong Pharmaceutical Co Ltd glp-1 receptor agonist and use thereof
US12441707B2 (en) 2019-12-30 2025-10-14 Tyra Biosciences, Inc. Indazole compounds
PL4097097T3 (pl) 2020-01-29 2025-05-12 Gilead Sciences, Inc. Związki modulujące glp-1r
KR102563111B1 (ko) * 2020-03-18 2023-08-04 주식회사 엘지화학 Glp-1 수용체 효능제, 이를 포함하는 약학적 조성물 및 이의 제조방법
WO2021187886A1 (ko) * 2020-03-18 2021-09-23 주식회사 엘지화학 Glp-1 수용체 효능제, 이를 포함하는 약학적 조성물 및 이의 제조방법
EP4196118A1 (en) 2020-08-13 2023-06-21 Boehringer Ingelheim International GmbH Treatment of cognitive impairement associated with schizophrenia
CA3195702A1 (en) 2020-10-13 2022-04-21 Boehringer Ingelheim International Gmbh Process of reworking
AU2021381323A1 (en) * 2020-11-19 2023-06-22 Cerecin Inc. Radiopharmaceutical ketone and dual tracer imaging in alzheimer's disease, cognitive impairment, and other conditions of altered cerebral metabolism
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
PE20240687A1 (es) 2020-12-30 2024-04-10 Tyra Biosciences Inc Compuestos de indazol como inhibidores de cinasas
US12180197B2 (en) 2021-03-11 2024-12-31 Gilead Sciences, Inc. GLP-1R modulating compounds
PE20240890A1 (es) 2021-05-13 2024-04-24 Carmot Therapeutics Inc Moduladores de los receptores acoplados a proteinas g
JP2024524883A (ja) 2021-06-09 2024-07-09 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物的に活性なジアジン－アミド化合物
TW202317534A (zh) * 2021-06-16 2023-05-01 美商西建公司 用於治療神經退化性疾病之含羧酸吖丁啶基化合物
US12018015B2 (en) 2021-06-18 2024-06-25 Aligos Therapeutics, Inc. Methods and compositions for targeting PD-L1
FI4408840T3 (fi) 2021-09-27 2025-11-04 Terns Pharmaceuticals Inc Bentsimidatsolikarboksyylihappoja glp-1r-agonisteina
EP4422745A1 (en) 2021-10-25 2024-09-04 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
US12428427B2 (en) 2021-12-16 2025-09-30 Aligos Therapeutics, Inc. Methods and compositions for targeting PD-L1
CA3252943A1 (en) 2022-02-23 2023-08-31 Terns Pharmaceuticals Inc COMPOUNDS AS GLP-1R AGONISTS
TWI866545B (zh) * 2022-10-20 2024-12-11 南韓商東亞Ｓｔ股份有限公司 氮雜環丁烷基苯并唑化合物及其等作為mer及axl抑制劑的用途
EP4568664A1 (en) 2023-04-07 2025-06-18 Terns Pharmaceuticals, Inc. Combination comprising a thr-beta agonist and a glp-1r agonist for use in treating a liver disorder or a cardiometabolic disease
WO2025147609A1 (en) * 2024-01-05 2025-07-10 Dewpoint Therapeutics, Inc. Amino quinoline compounds and uses thereof

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
UY27450A1 (es) 2001-09-24 2003-04-30 Bayer Corp Preparación y uso de derivados de imidazol para el tratamiento de la obesidad
EP1511710B1 (en) * 2002-05-31 2013-11-20 Proteotech, Inc. Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer s disease, type 2 diabetes, and parkinson s disease
US7582761B2 (en) 2002-10-17 2009-09-01 Amgen Inc. Vanilloid receptor ligands and their use in treatments
JP2007508241A (ja) 2003-07-31 2007-04-05 バイエル・フアーマシユーチカルズ・コーポレーシヨン Ｐｄｅ１０ａ阻害剤を用いる糖尿病および関連障害の処置方法
GB0325287D0 (en) 2003-10-29 2003-12-03 Merck Sharp & Dohme Therapeutic agents
PE20060241A1 (es) 2004-05-18 2006-04-01 Schering Corp 2-quinolil-oxazoles sustituidos como inhibidores de pde4
US20060019975A1 (en) 2004-07-23 2006-01-26 Pfizer Inc Novel piperidyl derivatives of quinazoline and isoquinoline
US20070072908A1 (en) * 2005-06-08 2007-03-29 Japan Tobacco Inc. Heterocyclic compounds
US7709501B2 (en) * 2005-12-23 2010-05-04 Amgen Inc. Vanilloid receptor ligands and their use in treatments
CA2635439A1 (en) 2006-01-27 2007-08-02 Pfizer Products Inc. Aminophthalazine derivative compounds
BRPI0821676A2 (pt) * 2007-12-21 2015-06-16 Astrazeneca Ab Composto, composição farmacêutica, e, processo para a preparação dos compostos.
BRPI0914891A2 (pt) 2008-06-20 2015-11-24 Metabolex Inc agonistas de aril gpr119 e usos dos mesmos
US20100041663A1 (en) * 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
SG176021A1 (en) * 2009-05-12 2011-12-29 Janssen Pharmaceuticals Inc 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
NZ598294A (en) 2009-09-03 2013-07-26 Bioenergenix Heterocyclic compounds for the inhibition of pask
EP2479165B1 (en) 2009-09-16 2017-10-25 Astellas Pharma Inc. Glycine compound
AU2011253058A1 (en) 2010-05-13 2012-12-06 Amgen Inc. Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
US8946230B2 (en) 2010-05-13 2015-02-03 Amgen Inc. Aryl- and heteroaryl- nitrogen-heterocyclic compounds as PDE10 inhibitors
JP2013526546A (ja) 2010-05-13 2013-06-24 アムジエン・インコーポレーテツド Ｐｄｅ１０阻害剤としてのヘテロアリ−ルオキシヘテロシクリル化合物
MA34300B1 (fr) * 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
UY34858A (es) * 2012-06-14 2013-11-29 Amgen Inc Compuestos de azetidina y piperidina útiles como inhibidores de pde10

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