CN115867536A - Gpr40激动剂 - Google Patents

Gpr40激动剂 Download PDF

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Publication number
CN115867536A
CN115867536A CN202180031973.XA CN202180031973A CN115867536A CN 115867536 A CN115867536 A CN 115867536A CN 202180031973 A CN202180031973 A CN 202180031973A CN 115867536 A CN115867536 A CN 115867536A
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CN
China
Prior art keywords
alkyl
independently
compound
pharmaceutically acceptable
prodrug
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Pending
Application number
CN202180031973.XA
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English (en)
Chinese (zh)
Inventor
伊雅苏·塞布哈特
何恕文
西蒙·马蒂厄
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Karyopp Ltd
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Karyopp Ltd
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Publication of CN115867536A publication Critical patent/CN115867536A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine 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
    • A61K31/435—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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/306—Arylalkanephosphinic acids, e.g. Ar-(CH2)n-P(=X)(R)(XH), (X = O,S, Se; n>=1)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/650952—Six-membered rings having the nitrogen atoms in the positions 1 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
CN202180031973.XA 2020-02-28 2021-02-26 Gpr40激动剂 Pending CN115867536A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US202062983438P 2020-02-28 2020-02-28
US62/983,438 2020-02-28
US202063076113P 2020-09-09 2020-09-09
US63/076,113 2020-09-09
US202063117074P 2020-11-23 2020-11-23
US63/117,074 2020-11-23
US202163147982P 2021-02-10 2021-02-10
US63/147,982 2021-02-10
PCT/US2021/019973 WO2021174046A1 (en) 2020-02-28 2021-02-26 Gpr40 agonists

Publications (1)

Publication Number Publication Date
CN115867536A true CN115867536A (zh) 2023-03-28

Family

ID=77490353

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180031973.XA Pending CN115867536A (zh) 2020-02-28 2021-02-26 Gpr40激动剂

Country Status (9)

Country Link
US (1) US20230151037A1 (https=)
EP (1) EP4110760A4 (https=)
JP (1) JP2023528713A (https=)
CN (1) CN115867536A (https=)
AU (1) AU2021225966A1 (https=)
CA (1) CA3173732A1 (https=)
TW (1) TW202140424A (https=)
UY (1) UY39106A (https=)
WO (1) WO2021174046A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116178281A (zh) * 2023-04-27 2023-05-30 中国药科大学 一种双功能免疫抑制剂及其制备方法和应用

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220150270A (ko) 2019-10-07 2022-11-10 칼리오페, 인크. Gpr119 효능제
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
EP4337202A4 (en) 2021-06-18 2025-04-02 Aligos Therapeutics, Inc. METHODS AND COMPOSITIONS FOR TARGETING PD-L1
EP4448512A4 (en) 2021-12-16 2025-11-19 Aligos Therapeutics Inc METHODS AND COMPOSITIONS FOR TARGETING PD-L1
CN118724767A (zh) * 2023-03-28 2024-10-01 南京华狮新材料有限公司 一种氨基酸衍生物及其制备方法和作为中间体合成l-草铵膦的方法
WO2025136929A1 (en) * 2023-12-19 2025-06-26 Kallyope, Inc. Gpr40 agonists
WO2025137310A1 (en) * 2023-12-22 2025-06-26 Kallyope, Inc. Crystalline gpr40 agonist and methods of making
WO2026019701A1 (en) * 2024-07-15 2026-01-22 Venenum Biodesign, LLC Substituted phenylsulfonamides as mgat2 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101501051A (zh) * 2006-08-23 2009-08-05 诺瓦提斯公司 作为神经磷脂酶抑制剂的酰胺化合物
WO2012011125A1 (en) * 2010-07-23 2012-01-26 Connexios Life Sciences Pvt. Ltd. Agonists of gpr40
US20150018422A1 (en) * 2012-02-13 2015-01-15 Takeda Pharmaceutical Company Limited Aromatic ring compound
US20160009662A1 (en) * 2014-07-09 2016-01-14 Janssen Pharmaceutica Nv Pyrazine gpr40 agonists for the treatment of type ii diabetes
WO2020242943A1 (en) * 2019-05-29 2020-12-03 Kallyope, Inc. Gpr40 agonists

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
CA2558585C (en) * 2004-02-27 2010-10-12 Amgen Inc. Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders
JP4875978B2 (ja) * 2004-03-15 2012-02-15 武田薬品工業株式会社 アミノフェニルプロパン酸誘導体
EP3076959B1 (en) * 2013-12-04 2018-07-04 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2015119899A1 (en) * 2014-02-06 2015-08-13 Merck Sharp & Dohme Corp. Antidiabetic compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101501051A (zh) * 2006-08-23 2009-08-05 诺瓦提斯公司 作为神经磷脂酶抑制剂的酰胺化合物
WO2012011125A1 (en) * 2010-07-23 2012-01-26 Connexios Life Sciences Pvt. Ltd. Agonists of gpr40
US20150018422A1 (en) * 2012-02-13 2015-01-15 Takeda Pharmaceutical Company Limited Aromatic ring compound
US20160009662A1 (en) * 2014-07-09 2016-01-14 Janssen Pharmaceutica Nv Pyrazine gpr40 agonists for the treatment of type ii diabetes
WO2020242943A1 (en) * 2019-05-29 2020-12-03 Kallyope, Inc. Gpr40 agonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SANATH K. MEEGALLA，等: "Discovery of a novel potent GPR40 full agonist", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 28, 12 January 2018 (2018-01-12), pages 720 - 726, XP055757324, DOI: 10.1016/j.bmcl.2018.01.013 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116178281A (zh) * 2023-04-27 2023-05-30 中国药科大学 一种双功能免疫抑制剂及其制备方法和应用
CN116178281B (zh) * 2023-04-27 2023-07-21 中国药科大学 一种双功能免疫抑制剂及其制备方法和应用

Also Published As

Publication number Publication date
WO2021174046A1 (en) 2021-09-02
AU2021225966A1 (en) 2022-09-15
TW202140424A (zh) 2021-11-01
EP4110760A4 (en) 2024-09-18
JP2023528713A (ja) 2023-07-06
EP4110760A1 (en) 2023-01-04
US20230151037A1 (en) 2023-05-18
CA3173732A1 (en) 2021-09-02
UY39106A (es) 2021-09-30

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