TW201623286A - 作為ｇｐｒ１１９調控劑用於治療糖尿病、肥胖、血脂異常及相關病症之異吲哚啉酮化合物 - Google Patents

作為ｇｐｒ１１９調控劑用於治療糖尿病、肥胖、血脂異常及相關病症之異吲哚啉酮化合物 Download PDF

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TW201623286A
TW201623286A TW104110614A TW104110614A TW201623286A TW 201623286 A TW201623286 A TW 201623286A TW 104110614 A TW104110614 A TW 104110614A TW 104110614 A TW104110614 A TW 104110614A TW 201623286 A TW201623286 A TW 201623286A
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Taiwan
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oxo
alkyl
oxy
pyrrolidin
pyridyl
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TW104110614A
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Chinese (zh)
Inventor
羅拉 施溫克
克利斯欽 邦尼
海納 葛隆畢克
馬提亞斯 高索
迪特 卡德瑞特
尼斯 哈蘭德
馬提亞斯 洛曼
克里斯多夫 波維連
科特 里德
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賽諾菲公司
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    • 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
    • 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
    • A61K31/40—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
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A—HUMAN NECESSITIES
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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
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
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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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
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    • 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
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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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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    • 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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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Diabetes (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW104110614A 2014-04-04 2015-04-01 作為ｇｐｒ１１９調控劑用於治療糖尿病、肥胖、血脂異常及相關病症之異吲哚啉酮化合物 TW201623286A (zh)

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US (1) US9908868B2 (enExample)
EP (1) EP3126350B1 (enExample)
JP (1) JP2017509678A (enExample)
KR (1) KR20160132415A (enExample)
CN (1) CN106164068A (enExample)
AR (1) AR099937A1 (enExample)
AU (1) AU2015239022A1 (enExample)
CA (1) CA2943864A1 (enExample)
CL (1) CL2016002498A1 (enExample)
DO (1) DOP2016000226A (enExample)
EA (1) EA201692007A1 (enExample)
EC (1) ECSP16078782A (enExample)
IL (1) IL248130A0 (enExample)
MA (1) MA39359A1 (enExample)
MX (1) MX2016013037A (enExample)
PE (1) PE20170333A1 (enExample)
PH (1) PH12016501724A1 (enExample)
SG (1) SG11201607247TA (enExample)
TW (1) TW201623286A (enExample)
WO (1) WO2015150565A1 (enExample)

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AP2016009521A0 (en) 2014-04-04 2016-10-31 Lundbeck & Co As H Halogenated quinazolin-thf-amines as pde1 inhibitors
CN105399744B (zh) * 2015-12-17 2017-07-18 黄燕鸽 一种奥格列汀的合成方法
CN110225752B (zh) 2016-09-12 2023-05-05 整体健康 用作gpr120调节器的单环化合物
CA3041038A1 (en) 2016-09-12 2018-03-15 Numerate, Inc. Bicyclic compounds useful as gpr120 modulators
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
US10392366B2 (en) 2017-02-21 2019-08-27 Sanofi Azetidine compounds as GPR119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders
CA3054452A1 (en) * 2017-03-14 2018-09-20 Dana-Farber Cancer Institute, Inc. Small molecule sensitization of bax activation for induction of cell death
IT201700039562A1 (it) * 2017-04-10 2018-10-10 Univ Pisa Derivati isoindolinici quali attivatori di ampk
TWI714231B (zh) * 2018-09-04 2020-12-21 美商美國禮來大藥廠 2,6-二胺基吡啶化合物
PH12022552277A1 (en) 2020-02-28 2024-03-04 Kallyope Inc Gpr40 agonists
KR102289381B1 (ko) * 2020-03-17 2021-08-17 주식회사 대웅테라퓨틱스 당뇨치료제 및 고지혈증 치료제를 포함하는 약학적 조성물
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
CN117164597B (zh) * 2023-11-02 2024-02-09 深圳创元生物医药科技有限公司 一种smtp-0合成方法

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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
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TW201623286A (zh) 2014-04-04 2016-07-01 賽諾菲公司 作為ｇｐｒ１１９調控劑用於治療糖尿病、肥胖、血脂異常及相關病症之異吲哚啉酮化合物

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WO2015150565A1 (en) 2015-10-08
US9908868B2 (en) 2018-03-06
MX2016013037A (es) 2017-01-09
US20170022182A1 (en) 2017-01-26
ECSP16078782A (es) 2017-02-24
AU2015239022A1 (en) 2016-10-13
MA39359A1 (fr) 2017-09-29
DOP2016000226A (es) 2016-10-31
JP2017509678A (ja) 2017-04-06
CA2943864A1 (en) 2015-10-08
IL248130A0 (en) 2016-11-30
KR20160132415A (ko) 2016-11-18
PE20170333A1 (es) 2017-04-21
EP3126350A1 (en) 2017-02-08
AR099937A1 (es) 2016-08-31
EP3126350B1 (en) 2018-07-04
CN106164068A (zh) 2016-11-23
PH12016501724A1 (en) 2016-10-03
SG11201607247TA (en) 2016-09-29
CL2016002498A1 (es) 2017-07-21
EA201692007A1 (ru) 2017-02-28

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