JP2017509679A - 糖尿病、肥満、脂質異常症および関連障害の治療のためのｇｐｒ１１９モジュレーターとしての置換縮合複素環 - Google Patents

糖尿病、肥満、脂質異常症および関連障害の治療のためのｇｐｒ１１９モジュレーターとしての置換縮合複素環 Download PDF

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JP2017509679A
JP2017509679A JP2016560725A JP2016560725A JP2017509679A JP 2017509679 A JP2017509679 A JP 2017509679A JP 2016560725 A JP2016560725 A JP 2016560725A JP 2016560725 A JP2016560725 A JP 2016560725A JP 2017509679 A JP2017509679 A JP 2017509679A
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Prior art keywords
alkyl
membered
inhibitor
oxo
cycloalkyl
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Abandoned
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JP2016560725A
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Japanese (ja)
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JP2017509679A5 (enExample
Inventor
ローター・シュヴィンク
クリスティアン・ブニング
ハイナー・グロンビク
マティアス・ゴッセル
ディーター・カーデライト
ニス・ハランド
マティーアス・ローマン
クリストフ・ペファーライン
クルト・リッター
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Sanofi SA
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Sanofi SA
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Publication of JP2017509679A publication Critical patent/JP2017509679A/ja
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    • 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
    • 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
    • C07D401/14—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016560725A 2014-04-04 2015-04-02 糖尿病、肥満、脂質異常症および関連障害の治療のためのｇｐｒ１１９モジュレーターとしての置換縮合複素環 Abandoned JP2017509679A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14305494 2014-04-04
EP14305494.8 2014-04-04
PCT/EP2015/057414 WO2015150564A1 (en) 2014-04-04 2015-04-02 Substituted fused heterocycles as gpr119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders

Publications (2)

Publication Number Publication Date
JP2017509679A true JP2017509679A (ja) 2017-04-06
JP2017509679A5 JP2017509679A5 (enExample) 2018-05-17

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JP2016560725A Abandoned JP2017509679A (ja) 2014-04-04 2015-04-02 糖尿病、肥満、脂質異常症および関連障害の治療のためのｇｐｒ１１９モジュレーターとしての置換縮合複素環

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Country Link
US (1) US9758520B2 (enExample)
EP (1) EP3126336B1 (enExample)
JP (1) JP2017509679A (enExample)
KR (1) KR20160132885A (enExample)
CN (1) CN106164073A (enExample)
AR (1) AR099936A1 (enExample)
AU (1) AU2015239021A1 (enExample)
CA (1) CA2942753A1 (enExample)
CL (1) CL2016002497A1 (enExample)
CR (1) CR20160460A (enExample)
DO (1) DOP2016000212A (enExample)
EA (1) EA030410B1 (enExample)
EC (1) ECSP16078779A (enExample)
IL (1) IL248129A0 (enExample)
MA (1) MA39346B1 (enExample)
MX (1) MX2016013033A (enExample)
PE (1) PE20161378A1 (enExample)
PH (1) PH12016501619A1 (enExample)
SG (1) SG11201606758SA (enExample)
TW (1) TW201625605A (enExample)
WO (1) WO2015150564A1 (enExample)

Families Citing this family (12)

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AP2016009521A0 (en) 2014-04-04 2016-10-31 Lundbeck & Co As H Halogenated quinazolin-thf-amines as pde1 inhibitors
TW201625605A (zh) 2014-04-04 2016-07-16 賽諾菲公司 用於治療糖尿病、肥胖、血脂異常及相關病症之作為ｇｐｒ１１９調節劑的經取代之稠合雜環類
TWI784968B (zh) 2016-09-09 2022-12-01 丹麥商西蘭製藥公司 澱粉素類似物
US10392366B2 (en) 2017-02-21 2019-08-27 Sanofi Azetidine compounds as GPR119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders
WO2019043635A1 (en) 2017-09-01 2019-03-07 Richter Gedeon Nyrt. COMPOUNDS INHIBITING THE ACTIVITY OF D-AMINO ACID OXIDASE
JP7265276B2 (ja) * 2018-05-31 2023-04-26 華領医薬技術（上海）有限公司 グルコキナーゼ活性化剤およびｓｇｌｔ－２阻害薬を含む医薬品の組合せ、組成物、配合剤、ならびにその調製方法および使用
KR102131359B1 (ko) * 2018-09-07 2020-07-07 오토텔릭바이오 주식회사 안정성이 향상된 의약 조성물
EP3976053A4 (en) * 2019-05-31 2022-11-23 Avolynt COMPOSITIONS AND METHODS OF TREATING A METABOLIC DISEASE
JP7502811B2 (ja) * 2019-11-05 2024-06-19 レスバーロジックス コーポレイション Ｂｅｔブロモドメイン阻害物質およびナトリウム依存性グルコース輸送体２阻害物質の組み合わせで主要な心血管有害事象（ｍａｃｅ）を処置および／または予防する方法
PH12022552277A1 (en) 2020-02-28 2024-03-04 Kallyope Inc Gpr40 agonists
CA3178994A1 (en) 2020-05-19 2021-11-25 Iyassu Sebhat Ampk activators
JP2023531726A (ja) 2020-06-26 2023-07-25 キャリーオペ，インク． Ａｍｐｋアクチベーター

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BRPI0410561A (pt) * 2003-06-18 2006-06-20 Pfizer Prod Inc lactamas de piperazinileteroarilóxi-n-arill e de piperazinilarilóxi
KR101055576B1 (ko) * 2006-04-21 2011-08-08 일라이 릴리 앤드 캄파니 11-베타-히드록시스테로이드 데히드로게나제 1의 억제제로서의 시클로헥실피라졸-락탐 유도체
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8299070B2 (en) * 2009-11-25 2012-10-30 Japan Tobacco Inc. Indole compounds and pharmaceutical use thereof
BR112012029395A2 (pt) * 2010-05-17 2016-07-26 Array Biopharma Inc lactamas piperdinil-substituídas como moduladores de gpr119
AU2011202239C1 (en) 2010-05-19 2017-03-16 Sanofi Long-acting formulations of insulins
JP2013537234A (ja) 2010-09-17 2013-09-30 アレイ バイオファーマ、インコーポレイテッド Ｇｐｒ１１９モジュレーターとしてのピペリジニル置換ラクタム
CA2853784A1 (en) 2011-11-11 2013-05-16 Glaxosmithkline Llc Treatment of blood lipid abnormalities and other conditions
TW201625605A (zh) 2014-04-04 2016-07-16 賽諾菲公司 用於治療糖尿病、肥胖、血脂異常及相關病症之作為ｇｐｒ１１９調節劑的經取代之稠合雜環類

Also Published As

Publication number Publication date
SG11201606758SA (en) 2016-09-29
EP3126336A1 (en) 2017-02-08
ECSP16078779A (es) 2017-02-24
MX2016013033A (es) 2017-01-09
CA2942753A1 (en) 2015-10-08
AU2015239021A1 (en) 2016-10-13
CL2016002497A1 (es) 2017-03-31
KR20160132885A (ko) 2016-11-21
IL248129A0 (en) 2016-11-30
TW201625605A (zh) 2016-07-16
PE20161378A1 (es) 2016-12-26
EA201692008A1 (ru) 2017-02-28
PH12016501619A1 (en) 2017-02-06
US20170022198A1 (en) 2017-01-26
US9758520B2 (en) 2017-09-12
DOP2016000212A (es) 2016-11-15
CR20160460A (es) 2017-02-21
EA030410B1 (ru) 2018-07-31
MA39346A1 (fr) 2017-09-29
CN106164073A (zh) 2016-11-23
MA39346B1 (fr) 2019-03-29
AR099936A1 (es) 2016-08-31
EP3126336B1 (en) 2018-12-05
WO2015150564A1 (en) 2015-10-08

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