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AR096339A1 - Agonistas del receptor de somatostatina subtipo 4 (sstr4) - Google Patents

Agonistas del receptor de somatostatina subtipo 4 (sstr4)

Info

Publication number
AR096339A1
AR096339A1 ARP140101981A ARP140101981A AR096339A1 AR 096339 A1 AR096339 A1 AR 096339A1 AR P140101981 A ARP140101981 A AR P140101981A AR P140101981 A ARP140101981 A AR P140101981A AR 096339 A1 AR096339 A1 AR 096339A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
group
monocyclic
bicyclic
Prior art date
Application number
ARP140101981A
Other languages
English (en)
Inventor
Ferrara Marco
Just Stefan
Kuelzer Raimund
Lingard Iain
Mazzaferro Rocco
Rudolf Klaus
Giovannini Riccardo
Cui Yunhai
Doods Henri
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR096339A1 publication Critical patent/AR096339A1/es

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    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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    • C—CHEMISTRY; METALLURGY
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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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D487/04—Ortho-condensed systems

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de la amida del ácido 3-aza-biciclo[3.1.0]hexan-6-carboxílico de la fórmula general (1), que son agonistas del receptor de somatostatina subtipo 4 (SSTR4), útiles para la prevención o el tratamiento de trastornos médicos relacionados con SSTR4. Además, procesos para preparar composiciones farmacéuticas, así como procesos para la fabricación de compuestos de acuerdo con la presente. Reivindicación 1: Compuestos caracterizados por la fórmula (1) en donde A se selecciona del grupo que consiste en H y alquilo C₁₋₆; R¹ y R² se seleccionan independientemente del grupo que consiste en H, alquilo C₁₋₆ y cicloalquilo C₃₋₆, en donde al menos uno de R¹ o R² es alquilo C₁₋₆ o cicloalquilo C₃₋₆, en donde alquilo C₁₋₆ o cicloalquilo C₃₋₆ se sustituyen opcionalmente con halógenos o MeO-, o en donde R¹ y R² juntos forman un puente de alquileno de 2 a 5 miembros opcionalmente sustituido con halógenos, que incorpora de 0 a 2 heteroátomos que se seleccionan independientemente del grupo que consiste en N, O y S; W se selecciona del grupo que consiste en arilo monocíclico o bicíclico, heteroarilo monocíclico o bicíclico, heterociclilo monocíclico o bicíclico, y cicloalquilo monocíclico o bicíclico, en donde cada uno de estos sistemas de anillos se sustituye opcionalmente con uno o más R³; y en donde el heteroarilo comprende hasta 4 heteroátomos y uno o dos anillos de 5 ó 6 miembros; R³ se selecciona independientemente del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₈, alquil C₁₋₆-O-, bencilo, halógeno, HO-, NC-, heteroarilo monocíclico o bicíclico, y heterociclilo monocíclico de 5 ó 6 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N, O ó S(O)ʳ, en donde el heteroarilo contiene hasta 4 heteroátomos y uno o dos anillos de 5 ó 6 miembros, y r es 0, 1 ó 2, en donde alquilo C₁₋₆, cicloalquilo C₃₋₈, alquil C₁₋₆-O-, bencilo, heteroarilo y heterociclilo se sustituyen opcionalmente con halógenos, HO-, acetilo, alquil C₁₋₆-O-, oxo, R⁴-S(O)₂-, en donde R⁴ es arilo, cicloalquilo C₃₋₆ y/o alquilo C₁₋₆; Y se selecciona del grupo que consiste en un enlace, -CH₂-, -CH₂CH₂- y -CH₂O-; o una sal de cualquiera de los compuestos mencionados anteriormente.
ARP140101981A 2013-05-17 2014-05-16 Agonistas del receptor de somatostatina subtipo 4 (sstr4) AR096339A1 (es)

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Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9371282B2 (en) 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists
MX385187B (es) 2013-05-17 2025-03-14 Incyte Holdings Corp Derivados del bipirazol como inhibidores de janus cinasa (jak)
EP3193875B1 (en) 2014-09-15 2022-02-16 Inflammatory Response Research, Inc. Levocetirizine and montelukast in the treatment of inflammation mediated conditions
JP6590927B2 (ja) * 2014-11-14 2019-10-16 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ソマトスタチン受容体サブタイプ４（ｓｓｔｒ４）作動薬としてのアリール及びヘテロアリール縮合テトラヒドロ−１，４−オキサゼピンアミド
MD3397631T2 (ro) 2015-12-29 2021-08-31 Pfizer 3-Azabiciclo[3.1.0] hexani substituiţi drept inhibitori de cetohexokinază
US11912687B2 (en) 2017-05-12 2024-02-27 Board of Trustees of the Southern Illinois University 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
EP3634406B1 (en) 2017-05-12 2023-09-06 Board of Trustees of The Southern Illinois University on behalf of Southern Illinois University Edwardsville 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
US10865163B2 (en) 2017-12-20 2020-12-15 The University Of Toledo Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds
BR112020016628A2 (pt) 2018-02-16 2020-12-15 Incyte Corporation Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
TWI834637B (zh) 2018-03-01 2024-03-11 日商武田藥品工業有限公司 六氫吡啶基-3-(芳氧基)丙醯胺及丙酸酯
MY206999A (en) 2018-03-30 2025-01-23 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
US11668295B2 (en) 2018-12-28 2023-06-06 Avent, Inc. Pump head for a peristaltic pump
CN112979655A (zh) 2019-12-16 2021-06-18 上海赛默罗生物科技有限公司 三唑并哒嗪类衍生物、其制备方法、药物组合物和用途
AR121682A1 (es) 2020-03-31 2022-06-29 Takeda Pharmaceuticals Co Derivados de n-(heterociclil y heterociclilalquil)-3-bencilpiridin-2-amina como agonistas de sstr4
EP4153178A4 (en) 2020-05-19 2024-06-05 Irr, Inc. Levocetirizine and montelukast in the treatment of sepsis and symptoms thereof
WO2021233428A1 (zh) * 2020-05-21 2021-11-25 广州费米子科技有限责任公司 含氮饱和杂环化合物及其制备方法、药物组合物和应用
KR20230015333A (ko) * 2020-05-21 2023-01-31 광저우 페르미온 테크놀로지 씨오., 엘티디. 융합된 고리 화합물, 이의 제조 방법, 이의 약제학적 조성물 및 용도
PL4157831T3 (pl) 2020-06-02 2025-03-03 Incyte Corporation Sposoby wytwarzania inhibitora jak1
WO2022012534A1 (zh) * 2020-07-13 2022-01-20 广州费米子科技有限责任公司 含氮杂环化合物、药物组合物和应用
US20230287322A1 (en) 2020-07-28 2023-09-14 Seagen Inc. Methods and systems for producing polypeptides
MX2023006542A (es) 2020-12-08 2023-08-25 Incyte Corp Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del vitiligo.
FI4333840T3 (fi) 2021-05-03 2025-12-12 Incyte Corp Jak1-reitin estäjiä kyhmykutinan hoitoon
AR127055A1 (es) * 2021-09-14 2023-12-13 Lilly Co Eli Sales agonistas de sstr4
EP4676477A1 (en) 2023-03-10 2026-01-14 Eli Lilly And Company Methods for the preparation and dose regimens for use of sstr4 agonists and salts thereof
CN120897906A (zh) 2023-03-10 2025-11-04 伊莱利利公司 制备sstr4激动剂及其盐的方法
WO2024245077A1 (zh) * 2023-05-29 2024-12-05 武汉熙瑞医药科技有限公司 3-氮杂-双环[3.1.0]己烷衍生物、其制备方法及其应用
AU2024317179A1 (en) * 2023-08-02 2026-01-15 Boehringer Ingelheim International Gmbh (2s,5r)-5-(hydroxymethyl)morpholine-2-carboxamides as agonists of sstr4
WO2025096300A1 (en) 2023-10-30 2025-05-08 Eli Lilly And Company Novel methods for the preparation of 3-azabicylco[3.1,0]hexane-6-carboxamide derivatives
WO2025193591A1 (en) 2024-03-11 2025-09-18 Eli Lilly And Company Crystalline form of a tartrate salt of an sstr4 agonist
WO2025247982A1 (en) 2024-05-29 2025-12-04 Grünenthal GmbH Piperazines which act as sstr4 modulators
WO2026019827A1 (en) * 2024-07-16 2026-01-22 Eli Lilly And Company Methods for the removal of n-tosyl protecting group

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6159941A (en) 1996-05-14 2000-12-12 Novo Nordisk A/S Use of somatostatin agonists and antagonists for treating diseases related to the eye
US6355613B1 (en) 1996-07-31 2002-03-12 Peptor Limited Conformationally constrained backbone cyclized somatostatin analogs
US6057338A (en) 1997-04-04 2000-05-02 Merck & Co., Inc. Somatostatin agonists
US6063796A (en) 1997-04-04 2000-05-16 Merck & Co., Inc. Somatostatin agonists
US20100004339A1 (en) 2003-10-06 2010-01-07 Oy Juvantia Pharma Ltd. Somatostatin Receptor 1 and/or 4 Selective Agonists and Antagonists
FI20031454A0 (fi) 2003-10-06 2003-10-06 Juvantia Pharma Ltd Oy Selektiivisiä somatostatiinireseptori 1 ja/tai 4 -agonisteja ja -antagonisteja
US7473787B2 (en) * 2003-10-14 2009-01-06 Pfizer Inc Bicyclic [3.1.0] derivatives as glycine transporter inhibitors
WO2008075172A2 (en) 2006-12-19 2008-06-26 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
WO2010059922A1 (en) 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
US8835472B2 (en) 2010-09-02 2014-09-16 Boehringer Ingelheim International Gmbh Compounds, pharmaceutical compositions and uses thereof
EP2685828A4 (en) * 2011-03-17 2014-08-13 Merck Sharp & Dohme SUBSTITUTED 3-AZABICYCLO [3,1,0-] HEXAN DERIVATIVES AS CCR2 ANTAGONISTS
CN102675290B (zh) * 2011-03-18 2014-11-12 山东亨利医药科技有限责任公司 含有并环的二氢吡唑类化合物
KR101556318B1 (ko) * 2013-05-15 2015-10-01 한국과학기술연구원 칼슘이온 채널 조절제로서 유효한 6-피라졸일아미도-3-치환된 아자바이사이클로[3.1.0]헥산 유도체
US9371282B2 (en) * 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists

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