TW202528300A - 人類整合素α4β7拮抗劑 - Google Patents
人類整合素α4β7拮抗劑Info
- Publication number
- TW202528300A TW202528300A TW113137058A TW113137058A TW202528300A TW 202528300 A TW202528300 A TW 202528300A TW 113137058 A TW113137058 A TW 113137058A TW 113137058 A TW113137058 A TW 113137058A TW 202528300 A TW202528300 A TW 202528300A
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- methyl
- mmol
- group
- propanoate
- Prior art date
Links
Classifications
-
- 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
Landscapes
- 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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862656742P | 2018-04-12 | 2018-04-12 | |
| US62/656,742 | 2018-04-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW202528300A true TW202528300A (zh) | 2025-07-16 |
Family
ID=68161020
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW113137058A TW202528300A (zh) | 2018-04-12 | 2019-04-12 | 人類整合素α4β7拮抗劑 |
| TW108112877A TWI856956B (zh) | 2018-04-12 | 2019-04-12 | 人類整合素α４β７拮抗劑 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108112877A TWI856956B (zh) | 2018-04-12 | 2019-04-12 | 人類整合素α４β７拮抗劑 |
Country Status (8)
| Country | Link |
|---|---|
| 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=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7365358B2 (ja) * | 2018-04-12 | 2023-10-19 | モーフィック セラピューティック，インコーポレイテッド | ヒトインテグリンα４β７のアンタゴニスト |
| CN112969700B (zh) | 2018-10-30 | 2024-08-20 | 吉利德科学公司 | 作为α4β7整合素抑制剂的咪唑并吡啶衍生物 |
| KR102659859B1 (ko) | 2018-10-30 | 2024-04-25 | 길리애드 사이언시즈, 인코포레이티드 | 알파4β7 인테그린의 억제를 위한 화합물 |
| AU2019373242B2 (en) | 2018-10-30 | 2023-07-13 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| EP4541422A3 (en) | 2018-10-30 | 2025-06-25 | Gilead Sciences, Inc. | Quinoline derivatives as alpha4beta7 integrin inhibitors |
| KR102908219B1 (ko) | 2019-08-14 | 2026-01-08 | 길리애드 사이언시즈, 인코포레이티드 | 알파 4 베타 7 인테그린의 저해용 화합물 |
| WO2021076890A1 (en) * | 2019-10-16 | 2021-04-22 | Morphic Therapeutic, Inc. | INHIBITING HUMAN INTEGRIN α4β7 |
| IL302906A (en) * | 2020-11-20 | 2023-07-01 | Denali Therapeutics Inc | Compounds, compositions, and methods |
| CN118591535A (zh) * | 2021-12-27 | 2024-09-03 | 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 |
| JP2025530250A (ja) * | 2022-09-09 | 2025-09-11 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | プロピオン酸誘導体及びその医薬的な応用 |
| KR20250120367A (ko) * | 2022-12-22 | 2025-08-08 | 신테라, 인크. | 알파4 베타7 인테그린 안타고니스트 및 이의 용도 |
| JP2026506997A (ja) * | 2023-02-21 | 2026-02-27 | シーフォーエックス・ディスカバリー・リミテッド | 大環状アルファ４ベータ７インテグリン阻害剤 |
| WO2025026955A1 (en) * | 2023-07-28 | 2025-02-06 | Galapagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
| TW202515852A (zh) * | 2023-09-15 | 2025-04-16 | 美商莫菲克醫療股份有限公司 | 抑制人類整合素α４β７ |
| 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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| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| CA2159450C (en) * | 1993-03-31 | 2002-01-08 | Norman Anthony Abood | 1-amidinophenyl-pyrrolidones piperidinones azetinones as platelet aggregation inhibitors |
| DE4427979A1 (de) * | 1993-11-15 | 1996-02-15 | Cassella Ag | Substituierte 5-Ring-Heterocyclen, ihre Herstellung und ihre Verwendung |
| US5849736A (en) * | 1993-11-24 | 1998-12-15 | The Dupont Merck Pharmaceutical Company | Isoxazoline and isoxazole fibrinogen receptor antagonists |
| BR9408137A (pt) | 1993-11-24 | 1997-08-12 | Du Pont Merck Pharma | Composto éster de prodroga método de tratamento composição farmacêutica e método de inibição |
| DE19622489A1 (de) * | 1996-06-05 | 1997-12-11 | Hoechst Ag | Salze des 3-(2-(4-(4-(Amino-imino-methyl)-phenyl)-4- methyl-2,5-dioxo-imidazolidin-1-yl)-acetylamino)-3- phenyl-propionsäure-ethylesters |
| US5981546A (en) * | 1996-08-29 | 1999-11-09 | Merck & Co., Inc. | Integrin antagonists |
| WO1998016524A1 (en) | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | HETEROCYCLIC DERIVATIVES AS FACTOR Xa INHIBITORS |
| EP0932615A1 (en) | 1996-10-11 | 1999-08-04 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
| DE19751251A1 (de) * | 1997-11-19 | 1999-05-20 | Hoechst Marion Roussel De Gmbh | Substituierte Imidazolidinderivate, ihre Herstellung, ihre Verwendung und sie enthaltende pharmezeutische Präparate |
| US6645939B1 (en) | 1997-11-24 | 2003-11-11 | Merck & Co., Inc. | Substituted β-alanine derivatives as cell adhesion inhibitors |
| MY153569A (en) | 1998-01-20 | 2015-02-27 | Mitsubishi Tanabe Pharma Corp | Inhibitors of ?4 mediated cell adhesion |
| DE19821483A1 (de) * | 1998-05-14 | 1999-11-18 | Hoechst Marion Roussel De Gmbh | Imidazolidinderivate, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| CA2333647A1 (en) * | 1998-06-29 | 2000-01-06 | Dupont Pharmaceuticals Company | Cyclic carbamates and isoxazolidines as iib/iiia antagonists |
| GB9826174D0 (en) * | 1998-11-30 | 1999-01-20 | Celltech Therapeutics Ltd | Chemical compounds |
| US6972296B2 (en) | 1999-05-07 | 2005-12-06 | Encysive Pharmaceuticals Inc. | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors |
| US6723711B2 (en) * | 1999-05-07 | 2004-04-20 | Texas Biotechnology Corporation | Propanoic acid derivatives that inhibit the binding of integrins to their receptors |
| BR0010349B1 (pt) * | 1999-05-07 | 2011-10-04 | derivados de ácido propanóico que inibem a ligação de integrinas aos seus receptores. | |
| CA2385882C (en) | 1999-09-24 | 2009-11-24 | Genentech, Inc. | Tyrosine derivatives |
| DE10041423A1 (de) | 2000-08-23 | 2002-03-07 | Merck Patent Gmbh | Biphenylderivate |
| DE10111876A1 (de) * | 2001-03-10 | 2002-09-19 | Aventis Pharma Gmbh | Bis(trifluormethyl)hydantoine als Zwischenprodukte für pharmazeutische Wirkstoffe |
| DE10154280A1 (de) | 2001-11-05 | 2003-05-15 | Wilex Ag | Antagonisten für alpha¶4¶-Integrine |
| PL215263B1 (pl) | 2002-02-25 | 2013-11-29 | Elan Pharm Inc | Kompozycja do przewleklego leczenia patologicznego zapalenia i zastosowanie natalizumabu lub jego immunologicznie aktywnego fragmentu do wytwarzania leku |
| RS52213B (sr) | 2004-09-03 | 2012-10-31 | Genentech, Inc. | Humanizovani anti-beta7 antagonisti i njihove primene |
| ES2387317T3 (es) | 2005-03-03 | 2012-09-20 | Seedlings Life Science Ventures, Llc. | Procedimiento de control de riesgos de pacientes en tratamiento con natalizumab |
| WO2006126529A1 (ja) | 2005-05-25 | 2006-11-30 | Shionogi & Co., Ltd. | ６，７－不飽和－７－カルバモイル置換モルヒナン誘導体 |
| AU2006254772B2 (en) | 2005-06-09 | 2011-06-02 | Ucb Pharma S.A. | 2,6 quinolinyl derivatives, processes for preparing them and their use as medicament |
| ES2752137T3 (es) | 2006-02-28 | 2020-04-03 | Biogen Ma Inc | Métodos para tratar enfermedades inflamatorias y autoinmunes con natalizumab |
| US20100272680A1 (en) | 2009-02-09 | 2010-10-28 | Subramanian Baskaran | Piperidinyl Cyclic Amido Antiviral Agents |
| EP3412309A1 (en) | 2011-03-31 | 2018-12-12 | F. Hoffmann-La Roche AG | Methods of administering beta7 integrin antagonists |
| EP2903691B1 (en) | 2012-10-05 | 2019-05-22 | F.Hoffmann-La Roche Ag | Methods for diagnosing and treating inflammatory bowel disease |
| KR20220065091A (ko) | 2014-03-27 | 2022-05-19 | 제넨테크, 인크. | 염증성 장 질환의 진단 및 치료 방법 |
| WO2016011940A1 (zh) | 2014-07-25 | 2016-01-28 | 江苏恒瑞医药股份有限公司 | 氮茚-酰胺类衍生物、其制备方法及其在医药上的应用 |
| KR20170120601A (ko) | 2015-02-26 | 2017-10-31 | 제넨테크, 인크. | 인테그린 베타7 길항제 및 크론병을 치료하는 방법 |
| US10246451B2 (en) | 2017-04-26 | 2019-04-02 | Aviara Pharmaceuticals, Inc. | Propionic acid derivatives and methods of use thereof |
| JP7365358B2 (ja) | 2018-04-12 | 2023-10-19 | モーフィック セラピューティック，インコーポレイテッド | ヒトインテグリンα４β７のアンタゴニスト |
| AU2019373242B2 (en) | 2018-10-30 | 2023-07-13 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| KR102659859B1 (ko) | 2018-10-30 | 2024-04-25 | 길리애드 사이언시즈, 인코포레이티드 | 알파4β7 인테그린의 억제를 위한 화합물 |
| CN112969700B (zh) | 2018-10-30 | 2024-08-20 | 吉利德科学公司 | 作为α4β7整合素抑制剂的咪唑并吡啶衍生物 |
| EP4541422A3 (en) | 2018-10-30 | 2025-06-25 | Gilead Sciences, Inc. | Quinoline derivatives as alpha4beta7 integrin inhibitors |
| WO2021076890A1 (en) | 2019-10-16 | 2021-04-22 | Morphic Therapeutic, Inc. | INHIBITING HUMAN INTEGRIN α4β7 |
-
2019
- 2019-04-12 JP JP2020555323A patent/JP7365358B2/ja active Active
- 2019-04-12 EP EP19785592.7A patent/EP3773573B1/en active Active
- 2019-04-12 TW TW113137058A patent/TW202528300A/zh unknown
- 2019-04-12 TW TW108112877A patent/TWI856956B/zh active
- 2019-04-12 WO PCT/US2019/027141 patent/WO2019200202A1/en not_active Ceased
- 2019-04-12 US US16/382,512 patent/US10759756B2/en active Active
- 2019-04-12 CN CN201980033206.5A patent/CN112312910A/zh active Pending
- 2019-04-12 MA MA052249A patent/MA52249A/fr unknown
- 2019-04-12 AR ARP190100980A patent/AR114489A1/es unknown
-
2020
- 2020-07-27 US US16/939,812 patent/US11174228B2/en active Active
-
2021
- 2021-11-12 US US17/525,479 patent/US20220340529A1/en not_active Abandoned
-
2023
- 2023-10-06 JP JP2023174330A patent/JP7700193B2/ja active Active
- 2023-12-22 US US18/394,421 patent/US12221416B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN112312910A (zh) | 2021-02-02 |
| JP7700193B2 (ja) | 2025-06-30 |
| MA52249A (fr) | 2021-05-05 |
| US20240294475A1 (en) | 2024-09-05 |
| JP2024001201A (ja) | 2024-01-09 |
| US20220340529A1 (en) | 2022-10-27 |
| AR114489A1 (es) | 2020-09-09 |
| US20200385352A1 (en) | 2020-12-10 |
| US12221416B2 (en) | 2025-02-11 |
| TWI856956B (zh) | 2024-10-01 |
| JP7365358B2 (ja) | 2023-10-19 |
| WO2019200202A1 (en) | 2019-10-17 |
| EP3773573A4 (en) | 2022-04-06 |
| US11174228B2 (en) | 2021-11-16 |
| EP3773573B1 (en) | 2026-03-18 |
| EP3773573A1 (en) | 2021-02-17 |
| TW202003466A (zh) | 2020-01-16 |
| US10759756B2 (en) | 2020-09-01 |
| JP2021531234A (ja) | 2021-11-18 |
| US20190315692A1 (en) | 2019-10-17 |
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