CN103649072A - 基于4h-噻吩并[3,2-c]色烯的背板胶质乙酰酯酶抑制剂及其用法 - Google Patents

基于4h-噻吩并[3,2-c]色烯的背板胶质乙酰酯酶抑制剂及其用法 Download PDF

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Publication number
CN103649072A
CN103649072A CN201280025844.0A CN201280025844A CN103649072A CN 103649072 A CN103649072 A CN 103649072A CN 201280025844 A CN201280025844 A CN 201280025844A CN 103649072 A CN103649072 A CN 103649072A
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China
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compound
alkyl
mmol
independently
acid
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Pending
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CN201280025844.0A
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English (en)
Chinese (zh)
Inventor
约瑟夫·巴博萨
肯尼斯·戈登·卡森
迈克尔·瓦尔特·加德彦
贾森·帕特里克·希利
韩强
罗斯·玛博恩
普拉温·帕巴
小詹姆斯·塔弗
克里斯滕·M·泰拉诺瓦
阿肖克·图努里
许小炼
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Lexicon Pharmaceuticals Inc
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Lexicon Genetics Inc
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Publication of CN103649072A publication Critical patent/CN103649072A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN201280025844.0A 2011-05-27 2012-05-23 基于4h-噻吩并[3,2-c]色烯的背板胶质乙酰酯酶抑制剂及其用法 Pending CN103649072A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161490839P 2011-05-27 2011-05-27
US61/490,839 2011-05-27
PCT/US2012/039087 WO2012166458A1 (en) 2011-05-27 2012-05-23 4h-thieno[3,2-c]chromene-based inhibitors of notum pectinacetylesterase and methods of their use

Publications (1)

Publication Number Publication Date
CN103649072A true CN103649072A (zh) 2014-03-19

Family

ID=46201840

Family Applications (1)

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CN201280025844.0A Pending CN103649072A (zh) 2011-05-27 2012-05-23 基于4h-噻吩并[3,2-c]色烯的背板胶质乙酰酯酶抑制剂及其用法

Country Status (12)

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US (2) US20120302562A1 (enExample)
EP (1) EP2714675B1 (enExample)
JP (1) JP6166718B2 (enExample)
CN (1) CN103649072A (enExample)
AU (1) AU2012262748B2 (enExample)
CA (1) CA2837084C (enExample)
DK (1) DK2714675T3 (enExample)
ES (1) ES2715832T3 (enExample)
HU (1) HUE043221T2 (enExample)
PL (1) PL2714675T3 (enExample)
PT (1) PT2714675T (enExample)
WO (1) WO2012166458A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108948011A (zh) * 2018-08-14 2018-12-07 华南农业大学 一种普拉多沙星的制备方法
CN109134493A (zh) * 2018-09-19 2019-01-04 浙江师范大学 一种具有抗菌活性的2-氧代色烯并噻吩衍生物及其合成方法和应用
CN112094182A (zh) * 2020-09-22 2020-12-18 中国海洋大学 一种医药中间体苯并环己酮化合物的绿色合成方法

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2012262748B2 (en) * 2011-05-27 2017-03-02 Lexicon Pharmaceuticals, Inc. 4H-thieno[3,2-c]chromene-based inhibitors of Notum Pectinacetylesterase and methods of their use
KR102836360B1 (ko) 2016-04-15 2025-07-23 베크만 컬터, 인코포레이티드 광활성 거대분자 및 그의 용도
WO2019044946A1 (ja) 2017-08-31 2019-03-07 第一三共株式会社 抗体－薬物コンジュゲートの新規製造方法
GB201814151D0 (en) 2018-08-31 2018-10-17 Ucl Business Plc Compounds

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3786064A (en) * 1969-04-05 1974-01-15 Bayer Ag Benzoxazole compounds useful as optical brightening agents
DE2628878A1 (de) * 1976-06-26 1978-01-05 Bayer Ag Beschichtungszusammensetzung
US4797414A (en) * 1985-02-23 1989-01-10 Zyma Sa Naphthothiophene derivatives and their use as respiratory enhancing agents
WO2000054769A1 (en) * 1999-03-16 2000-09-21 Smithkline Beecham Corporation Protease inhibitors
WO2006080406A1 (ja) * 2005-01-28 2006-08-03 Taisho Pharmaceutical Co., Ltd. 三環性化合物
US20060189678A1 (en) * 2003-07-31 2006-08-24 Minoru Taguchi 4,5-dihydronaphtho[1,2-b]thiophene derivative

Family Cites Families (8)

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Publication number Priority date Publication date Assignee Title
US4487778A (en) * 1983-01-27 1984-12-11 Fmc Corporation Insecticidal esters derived from benzocycloalkane-thiophenemethyl compounds
US6080576A (en) 1998-03-27 2000-06-27 Lexicon Genetics Incorporated Vectors for gene trapping and gene activation
FR2790959B1 (fr) 1999-03-15 2003-06-27 Pf Medicament Utilisation de fractions membranaires bacteriennes a effet adjuvant, leurs procedes de preparation et composition pharmaceutique les contenant
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
JP2005536518A (ja) 2002-07-19 2005-12-02 ファルマシア コーポレイション 炎症治療のための置換チオフェンカルボキサミド化合物
WO2006080439A1 (ja) * 2005-01-28 2006-08-03 Taisho Pharmaceutical Co., Ltd. 三環性化合物
RU2506267C2 (ru) * 2008-03-31 2014-02-10 Дженентек, Инк. Бензопирановые и бензоксепиновые ингибиторы рi3k и их применение
AU2012262748B2 (en) * 2011-05-27 2017-03-02 Lexicon Pharmaceuticals, Inc. 4H-thieno[3,2-c]chromene-based inhibitors of Notum Pectinacetylesterase and methods of their use

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3786064A (en) * 1969-04-05 1974-01-15 Bayer Ag Benzoxazole compounds useful as optical brightening agents
DE2628878A1 (de) * 1976-06-26 1978-01-05 Bayer Ag Beschichtungszusammensetzung
US4797414A (en) * 1985-02-23 1989-01-10 Zyma Sa Naphthothiophene derivatives and their use as respiratory enhancing agents
WO2000054769A1 (en) * 1999-03-16 2000-09-21 Smithkline Beecham Corporation Protease inhibitors
US20060189678A1 (en) * 2003-07-31 2006-08-24 Minoru Taguchi 4,5-dihydronaphtho[1,2-b]thiophene derivative
WO2006080406A1 (ja) * 2005-01-28 2006-08-03 Taisho Pharmaceutical Co., Ltd. 三環性化合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
E. CAMPAIGNE ET AL.: "A New Synthesis of Thiophenes and Condensed Thiophenes by Ring Closure of Disulfides", 《J. ORG. CHEM.》, vol. 21, 31 January 1956 (1956-01-31), pages 39 - 44 *
GARY L. GRUNEWALD ET AL.: "Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 15, 10 November 2006 (2006-11-10), pages 1298 - 1310, XP005823071, DOI: doi:10.1016/j.bmc.2006.11.010 *
S.K. PAL ET AL.: "Synthesis, characterization and laser flash photolysis studies of some naphthothiophenes bearing electron donor and acceptor functional groups", 《JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A: CHEMISTRY》, vol. 174, 4 May 2005 (2005-05-04), pages 138 - 148 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108948011A (zh) * 2018-08-14 2018-12-07 华南农业大学 一种普拉多沙星的制备方法
CN109134493A (zh) * 2018-09-19 2019-01-04 浙江师范大学 一种具有抗菌活性的2-氧代色烯并噻吩衍生物及其合成方法和应用
CN112094182A (zh) * 2020-09-22 2020-12-18 中国海洋大学 一种医药中间体苯并环己酮化合物的绿色合成方法

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Publication number Publication date
EP2714675B1 (en) 2019-01-02
EP2714675A1 (en) 2014-04-09
ES2715832T3 (es) 2019-06-06
CA2837084C (en) 2019-09-17
PT2714675T (pt) 2019-04-12
US20120302562A1 (en) 2012-11-29
US9624238B2 (en) 2017-04-18
US20140256784A1 (en) 2014-09-11
WO2012166458A1 (en) 2012-12-06
AU2012262748A1 (en) 2013-11-28
PL2714675T3 (pl) 2019-07-31
CA2837084A1 (en) 2012-12-06
JP6166718B2 (ja) 2017-07-19
HUE043221T2 (hu) 2019-08-28
AU2012262748B2 (en) 2017-03-02
JP2014517848A (ja) 2014-07-24
DK2714675T3 (en) 2019-04-15

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