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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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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    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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

Country Status (21)

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)

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CN106132953B (zh) 2014-04-04 2019-03-22 H.隆德贝克有限公司 作为pde1抑制剂的卤化的喹唑啉-thf-胺
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
AR109514A1 (es) 2016-09-09 2018-12-19 Zealand Pharma As Análogos de amilina
AR110988A1 (es) 2017-02-21 2019-05-22 Sanofi Sa Compuestos de azetidina como moduladores de gpr119 para el tratamiento de la diabetes, la obesidad, la dislipidemia y trastornos relacionados
WO2019043635A1 (en) 2017-09-01 2019-03-07 Richter Gedeon Nyrt. COMPOUNDS INHIBITING THE ACTIVITY OF D-AMINO ACID OXIDASE
LT3804714T (lt) * 2018-05-31 2025-03-10 Hua Medicine (Shanghai) Ltd. Farmacinis derinys ir kompozicija, ir derinio preparatas, kurio sudėtyje yra gliukokinazės aktyvatorius ir biguanido hipoglikeminis vaistas, taip pat jų gamybos būdas ir panaudojimas
KR102131359B1 (ko) * 2018-09-07 2020-07-07 오토텔릭바이오 주식회사 안정성이 향상된 의약 조성물
US11248001B2 (en) 2019-01-18 2022-02-15 Astrazeneca Ab PCSK9 inhibitors and methods of use thereof
EA202191890A1 (ru) 2019-01-18 2022-02-03 Астразенека Аб Ингибиторы pcsk9 и способы их применения
CN114450011B (zh) * 2019-05-31 2024-10-22 阿沃林特有限公司 用于治疗代谢性疾病的组合物和方法
TWI867086B (zh) * 2019-11-05 2024-12-21 加拿大商瑞斯弗洛吉克斯公司 以rvx-208及sglt2抑制劑治療及/或預防主要不良心血管事件(mace)的方法
CA3173731A1 (en) 2020-02-28 2021-09-02 Kallyope, Inc. Gpr40 agonists
CN116323608A (zh) 2020-05-19 2023-06-23 卡尔优普公司 Ampk活化剂
EP4172162A4 (en) 2020-06-26 2024-08-07 Kallyope, Inc. AMPK ACTIVATORS
JP7858636B2 (ja) 2020-09-10 2026-05-14 ガシャーブラム・バイオ・インコーポレイテッド ヘテロ環ｇｌｐ－１アゴニスト
MX2024005969A (es) 2022-05-30 2024-06-11 Zealand Pharma As Formulaciones liquidas de analogos de amilina.

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WO2004110994A1 (en) * 2003-06-18 2004-12-23 Pfizer Products Inc. Novel piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
CA2647677C (en) * 2006-04-21 2014-03-18 Eli Lilly And Company Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
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
SG185615A1 (en) * 2010-05-17 2012-12-28 Array Biopharma Inc Piperidinyl-substituted lactams as gpr119 modulators
AU2011202239C1 (en) 2010-05-19 2017-03-16 Sanofi Long-acting formulations of insulins
BR112013006344A2 (pt) 2010-09-17 2016-06-21 Array Biopharma Inc lactamas substituídas por piperdinila como moduladores de gpr119, composição farmacêutica as compreendendo, uso e processso para preparação das mesmas
EP2776039A2 (en) 2011-11-11 2014-09-17 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

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

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