CN112312910A - 人整合素α4β7拮抗剂 - Google Patents

人整合素α4β7拮抗剂 Download PDF

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Publication number
CN112312910A
CN112312910A CN201980033206.5A CN201980033206A CN112312910A CN 112312910 A CN112312910 A CN 112312910A CN 201980033206 A CN201980033206 A CN 201980033206A CN 112312910 A CN112312910 A CN 112312910A
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compound
methyl
group
alkyl
mixture
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CN201980033206.5A
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Chinese (zh)
Inventor
M·G·伯萨维奇
D·M·特罗亚斯特
B·A·哈里森
B·S·利帕
B·N·罗杰斯
K·D·康策
A·I·格拉休托
T·戴
林富扬
K·N·哈恩
M·A·斯文森
金丙澯
钟诚
A·A·卢戈夫斯科伊
B·索萨
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Murphy Medical Co ltd
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Murphy Medical Co ltd
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Publication of CN112312910A publication Critical patent/CN112312910A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • 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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
    • 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
    • C07D241/14—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 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
    • C07D241/18—Oxygen or sulfur atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Steroid Compounds (AREA)
CN201980033206.5A 2018-04-12 2019-04-12 人整合素α4β7拮抗剂 Pending CN112312910A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862656742P 2018-04-12 2018-04-12
US62/656742 2018-04-12
PCT/US2019/027141 WO2019200202A1 (en) 2018-04-12 2019-04-12 Antagonists of human integrin (alpha4)(beta7)

Publications (1)

Publication Number Publication Date
CN112312910A true CN112312910A (zh) 2021-02-02

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CN201980033206.5A Pending CN112312910A (zh) 2018-04-12 2019-04-12 人整合素α4β7拮抗剂

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US (4) US10759756B2 (https=)
EP (1) EP3773573B1 (https=)
JP (2) JP7365358B2 (https=)
CN (1) CN112312910A (https=)
AR (1) AR114489A1 (https=)
MA (1) MA52249A (https=)
TW (2) TW202528300A (https=)
WO (1) WO2019200202A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115087444A (zh) * 2019-10-16 2022-09-20 莫菲克医疗股份有限公司 抑制人整联蛋白α4β7
WO2023125182A1 (zh) * 2021-12-27 2023-07-06 海思科医药集团股份有限公司 一种丙酸衍生物及其在医药上的应用
WO2024051819A1 (zh) * 2022-09-09 2024-03-14 西藏海思科制药有限公司 一种丙酸衍生物及其在医药上的应用
WO2025176107A1 (zh) * 2024-02-20 2025-08-28 西藏海思科制药有限公司 一种吡啶酮衍生物及其在医药上的应用

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EP3773573B1 (en) * 2018-04-12 2026-03-18 Morphic Therapeutic, Inc. Antagonists of human integrin (alpha4)(beta7)
EP3873605B1 (en) 2018-10-30 2024-10-23 Gilead Sciences, Inc. Compounds for inhibition of alpha4beta7 integrin
FI3873884T3 (fi) 2018-10-30 2025-02-24 Gilead Sciences Inc 3-(kinolin-8-yyli)-1,4-dihydropyrido[3,4-d]pyrimidiini-2,4-dionijohdannaisia alfa-4-beta-7-integriinin estäjinä tulehdussairauksien hoidossa
JP7189368B2 (ja) 2018-10-30 2022-12-13 ギリアード サイエンシーズ， インコーポレイテッド アルファ４ベータ７インテグリンの阻害のための化合物
ES3013256T3 (en) 2018-10-30 2025-04-11 Gilead Sciences Inc Imidazo[1,2-a]pyridine derivatives as alpha4beta7 integrin inhibitors for the treatment of inflammatory diseases
WO2021030438A1 (en) 2019-08-14 2021-02-18 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
IL302906A (en) * 2020-11-20 2023-07-01 Denali Therapeutics Inc Compounds, compositions, and methods
JP2025542171A (ja) * 2022-12-22 2025-12-25 シンセラ， インコーポレイテッド アルファ４ベータ７インテグリンアンタゴニスト及びその使用
AU2024226489A1 (en) * 2023-02-21 2025-10-02 C4X Discovery Limited Macrocyclic alpha4beta7 integrin inhibitors
WO2025026955A1 (en) * 2023-07-28 2025-02-06 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
WO2025059417A1 (en) * 2023-09-15 2025-03-20 Morphic Therapeutic, Inc. INHIBITING HUMAN INTEGRIN α4β7

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CN1134696A (zh) * 1993-11-15 1996-10-30 赫彻斯特股份公司 取代的5-元杂环，它们的制备方法及用途
CN1202893A (zh) * 1995-05-31 1998-12-23 杜邦麦克药品公司 新的异噁唑啉和异噁唑纤维蛋白原受体拮抗剂
CN1225360A (zh) * 1997-11-19 1999-08-11 德国赫彻斯特马里奥罗塞尔有限公司 取代的咪唑烷衍生物,其制备、用途以及含有它们的药物制剂
US6667334B1 (en) * 1998-05-14 2003-12-23 Aventis Pharma Deutschland Gmbh Imidazolidine derivatives, the production thereof, their use and pharmaceutical preparations containing the same
WO2000000481A1 (en) * 1998-06-29 2000-01-06 Du Pont Pharmaceuticals Company Cyclic carbamates and isoxazolidines as iib/iiia antagonists
US6953798B1 (en) * 1998-11-30 2005-10-11 Celltech R&D Limited β-alanine derivates
US20030199692A1 (en) * 1999-05-07 2003-10-23 Biediger Ronald J. Propanoic acid derivatives that inhibit the binding of integrins to their receptors
US20020183374A1 (en) * 2001-03-10 2002-12-05 Volkmar Wehner Bis(trifluoromethyl)hydantoins as intermediates for pharmaceutically active ingredients

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115087444A (zh) * 2019-10-16 2022-09-20 莫菲克医疗股份有限公司 抑制人整联蛋白α4β7
CN115087444B (zh) * 2019-10-16 2024-09-17 莫菲克医疗股份有限公司 抑制人整联蛋白α4β7
WO2023125182A1 (zh) * 2021-12-27 2023-07-06 海思科医药集团股份有限公司 一种丙酸衍生物及其在医药上的应用
WO2024051819A1 (zh) * 2022-09-09 2024-03-14 西藏海思科制药有限公司 一种丙酸衍生物及其在医药上的应用
WO2025176107A1 (zh) * 2024-02-20 2025-08-28 西藏海思科制药有限公司 一种吡啶酮衍生物及其在医药上的应用

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MA52249A (fr) 2021-05-05
JP2024001201A (ja) 2024-01-09
TWI856956B (zh) 2024-10-01
US20220340529A1 (en) 2022-10-27
WO2019200202A1 (en) 2019-10-17
US11174228B2 (en) 2021-11-16
JP2021531234A (ja) 2021-11-18
US20190315692A1 (en) 2019-10-17
JP7700193B2 (ja) 2025-06-30
US20240294475A1 (en) 2024-09-05
EP3773573A4 (en) 2022-04-06
US20200385352A1 (en) 2020-12-10
EP3773573A1 (en) 2021-02-17
US12221416B2 (en) 2025-02-11
TW202528300A (zh) 2025-07-16
US10759756B2 (en) 2020-09-01
JP7365358B2 (ja) 2023-10-19
AR114489A1 (es) 2020-09-09
EP3773573B1 (en) 2026-03-18
TW202003466A (zh) 2020-01-16

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