TW201629057A - 新穎化合物αvβ整聯蛋白拮抗劑 - Google Patents

新穎化合物αvβ整聯蛋白拮抗劑 Download PDF

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Publication number
TW201629057A
TW201629057A TW104131367A TW104131367A TW201629057A TW 201629057 A TW201629057 A TW 201629057A TW 104131367 A TW104131367 A TW 104131367A TW 104131367 A TW104131367 A TW 104131367A TW 201629057 A TW201629057 A TW 201629057A
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Taiwan
Prior art keywords
compound
fluoro
formula
acid
mmol
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TW104131367A
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English (en)
Chinese (zh)
Inventor
尼爾 安德魯 安德森
克羅福德 馬修 霍華 詹姆斯 坎貝爾
艾西利 保羅 漢考克
約翰 馬丁 皮裘
喬安那 瑪莉 雷門
Original Assignee
葛蘭素史密斯克藍智慧財產發展有限公司
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Publication of TW201629057A publication Critical patent/TW201629057A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW104131367A 2014-09-26 2015-09-22 新穎化合物αvβ整聯蛋白拮抗劑 TW201629057A (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB1417011.2A GB201417011D0 (en) 2014-09-26 2014-09-26 Novel compounds

Publications (1)

Publication Number Publication Date
TW201629057A true TW201629057A (zh) 2016-08-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
TW104131367A TW201629057A (zh) 2014-09-26 2015-09-22 新穎化合物αvβ整聯蛋白拮抗劑

Country Status (15)

Country Link
US (1) US10000489B2 (OSRAM)
EP (1) EP3197893B1 (OSRAM)
JP (1) JP6665169B2 (OSRAM)
KR (1) KR20170063590A (OSRAM)
CN (1) CN107074849A (OSRAM)
AR (1) AR101995A1 (OSRAM)
AU (1) AU2015320859A1 (OSRAM)
BR (1) BR112017006253A2 (OSRAM)
CA (1) CA2962326A1 (OSRAM)
ES (1) ES2704525T3 (OSRAM)
GB (1) GB201417011D0 (OSRAM)
RU (1) RU2017114346A (OSRAM)
TW (1) TW201629057A (OSRAM)
UY (1) UY36315A (OSRAM)
WO (1) WO2016046226A1 (OSRAM)

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GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201604680D0 (en) * 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
GB201604681D0 (en) * 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
KR102506324B1 (ko) 2016-11-08 2023-03-03 브리스톨-마이어스 스큅 컴퍼니 알파 v 인테그린 억제제로서의 시클로부탄- 및 아제티딘-함유 모노 및 스피로시클릭 화합물
WO2018089357A1 (en) 2016-11-08 2018-05-17 Bristol-Myers Squibb Company INDAZOLE DERIVATIVES AS αV INTEGRIN ANTAGONISTS
CA3042693A1 (en) * 2016-11-08 2018-05-17 Bristol-Myers Squibb Company Pyrrole amides as .alpha.v integrin inhibitors
HRP20220990T1 (hr) 2016-11-08 2022-11-11 Bristol-Myers Squibb Company 3-supstituirane propionske kiseline kao inhibitori alfa v integrina
JP7128811B2 (ja) 2016-11-08 2022-08-31 ブリストル-マイヤーズ スクイブ カンパニー アルファvインテグリン阻害剤としてのアゾールアミドおよびアミン
US10696672B2 (en) 2016-12-23 2020-06-30 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
EP3589627A4 (en) 2017-02-28 2020-08-05 Morphic Therapeutic, Inc. (ALPHA-V) (BETA-6) INHIBITORS INTEGRIN
EP3760202A1 (en) 2017-02-28 2021-01-06 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
CN107823208A (zh) * 2017-10-25 2018-03-23 南京多宝生物科技有限公司 吗啉类化合物在制备治疗和预防肾纤维化药物中的应用
WO2019094319A1 (en) 2017-11-07 2019-05-16 Bristol-Myers Squibb Company Pyrrolopyrazine derivatives as alpha v integrin inhibitors
CN108208177A (zh) * 2017-11-28 2018-06-29 上海交通大学医学院附属新华医院 含丁酸类化合物的组合物及其应用
PL3844162T3 (pl) 2018-08-29 2025-06-09 Morphic Therapeutic, Inc. Inhibitory integryny alfa v beta 6
EP3617206A1 (en) 2018-08-29 2020-03-04 Morphic Therapeutic, Inc. Integrin inhibitors
TW202028179A (zh) * 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
WO2020074937A1 (en) * 2018-10-09 2020-04-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of alpha-v-integrin (cd51) inhibitors for the treatment of cardiac fibrosis
AU2019391097B2 (en) * 2018-12-04 2025-07-03 Sumitomo Pharma America, Inc. CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
EP4525866A1 (en) * 2022-05-18 2025-03-26 Pliant Therapeutics, Inc. Stabilization of integrin inhibitors
JP2025541280A (ja) 2022-12-14 2025-12-18 アルナイラム ファーマシューティカルズ, インコーポレイテッド 肝外送達のためのアルファ-vベータ-6(αvβ6)インテグリンリガンド
WO2025259743A1 (en) 2024-06-12 2025-12-18 Alnylam Pharmaceuticals, Inc. Dual conjugate compounds for extrahepatic delivery
WO2025259747A2 (en) 2024-06-12 2025-12-18 Alnylam Pharmaceuticals, Inc. Dystrophy myotonic protein kinase (dmpk) irna compositions and methods of use thereof

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Also Published As

Publication number Publication date
RU2017114346A (ru) 2018-11-02
EP3197893A1 (en) 2017-08-02
JP6665169B2 (ja) 2020-03-13
AU2015320859A1 (en) 2017-03-09
ES2704525T3 (es) 2019-03-18
UY36315A (es) 2016-04-29
US10000489B2 (en) 2018-06-19
US20170298063A1 (en) 2017-10-19
JP2017528503A (ja) 2017-09-28
BR112017006253A2 (pt) 2017-12-12
CA2962326A1 (en) 2016-03-31
GB201417011D0 (en) 2014-11-12
AR101995A1 (es) 2017-01-25
KR20170063590A (ko) 2017-06-08
CN107074849A (zh) 2017-08-18
EP3197893B1 (en) 2018-10-24
WO2016046226A1 (en) 2016-03-31

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