JP2020504120A - インテグリンアンタゴニスト - Google Patents
インテグリンアンタゴニスト Download PDFInfo
- Publication number
- JP2020504120A JP2020504120A JP2019534956A JP2019534956A JP2020504120A JP 2020504120 A JP2020504120 A JP 2020504120A JP 2019534956 A JP2019534956 A JP 2019534956A JP 2019534956 A JP2019534956 A JP 2019534956A JP 2020504120 A JP2020504120 A JP 2020504120A
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- alkyl
- compound
- integrin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 0 CN1C(OCCc2nc(NCCC3)c3cc2)=CC(CC(CC(*)=C)C(C=C(C2)Br)=CC2C2(CC2)C(F)F)*1 Chemical compound CN1C(OCCc2nc(NCCC3)c3cc2)=CC(CC(CC(*)=C)C(C=C(C2)Br)=CC2C2(CC2)C(F)F)*1 0.000 description 7
- CIKDYWXRZXYDDM-UHFFFAOYSA-N CC(C)(C)c(cc1C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)ccc1OC Chemical compound CC(C)(C)c(cc1C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)ccc1OC CIKDYWXRZXYDDM-UHFFFAOYSA-N 0.000 description 1
- JDAZWQYXNQSPIW-UHFFFAOYSA-N CC(C)(C)c1ccc(C(CC(OC=C)=O)Cc2n[n](C)c(OCCc3ccc(CCCN4)c4n3)c2)c(OC)c1 Chemical compound CC(C)(C)c1ccc(C(CC(OC=C)=O)Cc2n[n](C)c(OCCc3ccc(CCCN4)c4n3)c2)c(OC)c1 JDAZWQYXNQSPIW-UHFFFAOYSA-N 0.000 description 1
- QJZYIODCOIZZSL-UHFFFAOYSA-N CC(C)(C)c1ccc(C)c(C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)c1 Chemical compound CC(C)(C)c1ccc(C)c(C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)c1 QJZYIODCOIZZSL-UHFFFAOYSA-N 0.000 description 1
- CZQZQWSMKDKSBE-UHFFFAOYSA-N CC(C)(c1cc(Br)cc(OC(F)(F)F)c1)O Chemical compound CC(C)(c1cc(Br)cc(OC(F)(F)F)c1)O CZQZQWSMKDKSBE-UHFFFAOYSA-N 0.000 description 1
- IPXYLFBUULUDGA-UHFFFAOYSA-N C[n]1nc(CC(CC(O)=O)C(C=CC2OC)=CC2F)cc1OCCc1nc(NCCC2)c2cc1 Chemical compound C[n]1nc(CC(CC(O)=O)C(C=CC2OC)=CC2F)cc1OCCc1nc(NCCC2)c2cc1 IPXYLFBUULUDGA-UHFFFAOYSA-N 0.000 description 1
- FKCURGGUWZARNY-UHFFFAOYSA-N C[n]1nc(CC(CC(O)=O)c2cc(C#N)cc(C3(CC3)C(F)F)c2)cc1OCCc1ccc(CCCN2)c2n1 Chemical compound C[n]1nc(CC(CC(O)=O)c2cc(C#N)cc(C3(CC3)C(F)F)c2)cc1OCCc1ccc(CCCN2)c2n1 FKCURGGUWZARNY-UHFFFAOYSA-N 0.000 description 1
- TXXIRBSCDZTYCB-UHFFFAOYSA-N C[n]1nc(CC(CC(O)=O)c2cc(C3(CC3)C(F)F)cc(F)c2)cc1OCCc1nc(NCCC2)c2cc1 Chemical compound C[n]1nc(CC(CC(O)=O)c2cc(C3(CC3)C(F)F)cc(F)c2)cc1OCCc1nc(NCCC2)c2cc1 TXXIRBSCDZTYCB-UHFFFAOYSA-N 0.000 description 1
- TXXIRBSCDZTYCB-IBGZPJMESA-N C[n]1nc(C[C@@H](CC(O)=O)c2cc(C3(CC3)C(F)F)cc(F)c2)cc1OCCc1nc(NCCC2)c2cc1 Chemical compound C[n]1nc(C[C@@H](CC(O)=O)c2cc(C3(CC3)C(F)F)cc(F)c2)cc1OCCc1nc(NCCC2)c2cc1 TXXIRBSCDZTYCB-IBGZPJMESA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Ophthalmology & Optometry (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662440253P | 2016-12-29 | 2016-12-29 | |
| US62/440,253 | 2016-12-29 | ||
| US201762471882P | 2017-03-15 | 2017-03-15 | |
| US62/471,882 | 2017-03-15 | ||
| PCT/US2017/068801 WO2018132268A1 (en) | 2016-12-29 | 2017-12-28 | Integrin antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020504120A true JP2020504120A (ja) | 2020-02-06 |
| JP2020504120A5 JP2020504120A5 (enExample) | 2021-01-21 |
Family
ID=62840040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019534956A Pending JP2020504120A (ja) | 2016-12-29 | 2017-12-28 | インテグリンアンタゴニスト |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11306084B2 (enExample) |
| EP (1) | EP3562826A4 (enExample) |
| JP (1) | JP2020504120A (enExample) |
| KR (1) | KR20190100232A (enExample) |
| CN (1) | CN110177787A (enExample) |
| AU (1) | AU2017393297A1 (enExample) |
| BR (1) | BR112019012515A2 (enExample) |
| CA (1) | CA3045491A1 (enExample) |
| CO (1) | CO2019007023A2 (enExample) |
| IL (1) | IL267686A (enExample) |
| MX (1) | MX2019007797A (enExample) |
| PH (1) | PH12019501514A1 (enExample) |
| RU (1) | RU2019116820A (enExample) |
| WO (1) | WO2018132268A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190100232A (ko) | 2016-12-29 | 2019-08-28 | 세인트 루이스 유니버시티 | 인테그린 길항제 |
| EP3589285A4 (en) | 2017-02-28 | 2020-08-12 | Morphic Therapeutic, Inc. | INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6) |
| MA47697A (fr) | 2017-02-28 | 2020-01-08 | Morphic Therapeutic Inc | Inhibiteurs de l'(alpha-v)(bêta-6) intégrine |
| EP3617206A1 (en) | 2018-08-29 | 2020-03-04 | Morphic Therapeutic, Inc. | Integrin inhibitors |
| US20240245682A1 (en) * | 2022-12-27 | 2024-07-25 | Pliant Therapeutics, Inc. | Alpha-v-beta-8 integrin inhibitors and uses thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004511434A (ja) * | 2000-06-15 | 2004-04-15 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| JP2006513218A (ja) * | 2002-12-20 | 2006-04-20 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニスト誘導体としてのピラゾール化合物 |
| JP2006518333A (ja) * | 2002-12-20 | 2006-08-10 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| US20140051715A1 (en) * | 2012-07-18 | 2014-02-20 | Saint Louis University | 3,5 Phenyl-Substituted Beta Amino Acid Derivatives as Integrin Antagonists |
| JP2015524412A (ja) * | 2012-07-18 | 2015-08-24 | セントルイス ユニバーシティ | インテグリンアンタゴニストとしてのβアミノ酸誘導体 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1572690A1 (en) | 2002-12-20 | 2005-09-14 | Pharmacia Corporation | Thiazole compounds as integrin receptor antagonists derivatives |
| AU2014324426A1 (en) | 2013-09-30 | 2016-04-21 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| CA3042707A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | 3-substituted propionic acids as .alpha.v integrin inhibitors |
| KR102506327B1 (ko) | 2016-11-08 | 2023-03-03 | 브리스톨-마이어스 스큅 컴퍼니 | αV 인테그린 길항제로서의 인다졸 유도체 |
| 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 |
| LT3538528T (lt) | 2016-11-08 | 2021-03-10 | Bristol-Myers Squibb Company | Pirolo amidai, kaip alfa v integrino inhibitoriai |
| CN110167934B (zh) | 2016-11-08 | 2022-06-10 | 百时美施贵宝公司 | 作为αV整联蛋白抑制剂的含有环丁烷和含有氮杂环丁烷的单环和螺环化合物 |
| KR20190100232A (ko) | 2016-12-29 | 2019-08-28 | 세인트 루이스 유니버시티 | 인테그린 길항제 |
| EP3589285A4 (en) | 2017-02-28 | 2020-08-12 | Morphic Therapeutic, Inc. | INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6) |
| TWI841573B (zh) | 2018-06-27 | 2024-05-11 | 美商普萊恩醫療公司 | 具有未分支連接子之胺基酸化合物及使用方法 |
| US20210284638A1 (en) | 2018-07-03 | 2021-09-16 | Saint Louis University | ALPHAvBETA1 INTEGRIN ANTAGONISTS |
-
2017
- 2017-12-28 KR KR1020197019720A patent/KR20190100232A/ko not_active Withdrawn
- 2017-12-28 RU RU2019116820A patent/RU2019116820A/ru not_active Application Discontinuation
- 2017-12-28 AU AU2017393297A patent/AU2017393297A1/en not_active Abandoned
- 2017-12-28 CA CA3045491A patent/CA3045491A1/en not_active Abandoned
- 2017-12-28 CN CN201780080614.7A patent/CN110177787A/zh active Pending
- 2017-12-28 US US16/474,505 patent/US11306084B2/en active Active
- 2017-12-28 MX MX2019007797A patent/MX2019007797A/es unknown
- 2017-12-28 EP EP17891632.6A patent/EP3562826A4/en not_active Withdrawn
- 2017-12-28 BR BR112019012515-9A patent/BR112019012515A2/pt not_active Application Discontinuation
- 2017-12-28 JP JP2019534956A patent/JP2020504120A/ja active Pending
- 2017-12-28 WO PCT/US2017/068801 patent/WO2018132268A1/en not_active Ceased
-
2019
- 2019-06-26 IL IL267686A patent/IL267686A/en unknown
- 2019-06-27 PH PH12019501514A patent/PH12019501514A1/en unknown
- 2019-06-28 CO CONC2019/0007023A patent/CO2019007023A2/es unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004511434A (ja) * | 2000-06-15 | 2004-04-15 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| JP2006513218A (ja) * | 2002-12-20 | 2006-04-20 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニスト誘導体としてのピラゾール化合物 |
| JP2006518333A (ja) * | 2002-12-20 | 2006-08-10 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| US20140051715A1 (en) * | 2012-07-18 | 2014-02-20 | Saint Louis University | 3,5 Phenyl-Substituted Beta Amino Acid Derivatives as Integrin Antagonists |
| JP2015524412A (ja) * | 2012-07-18 | 2015-08-24 | セントルイス ユニバーシティ | インテグリンアンタゴニストとしてのβアミノ酸誘導体 |
Non-Patent Citations (1)
| Title |
|---|
| PENNING, THOMAS D. ET AL.: "Synthesis of pyrazoles and isoxazoles as potent αvβ3 receptor antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 12, JPN6021044729, 2006, pages 3156 - 3161, ISSN: 0004790851 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CA3045491A1 (en) | 2018-07-19 |
| BR112019012515A2 (pt) | 2019-11-19 |
| CO2019007023A2 (es) | 2019-07-31 |
| EP3562826A1 (en) | 2019-11-06 |
| PH12019501514A1 (en) | 2020-09-14 |
| IL267686A (en) | 2019-08-29 |
| US20190345155A1 (en) | 2019-11-14 |
| EP3562826A4 (en) | 2020-08-26 |
| WO2018132268A8 (en) | 2019-06-20 |
| KR20190100232A (ko) | 2019-08-28 |
| MX2019007797A (es) | 2019-10-21 |
| WO2018132268A1 (en) | 2018-07-19 |
| RU2019116820A (ru) | 2021-01-29 |
| US11306084B2 (en) | 2022-04-19 |
| CN110177787A (zh) | 2019-08-27 |
| AU2017393297A1 (en) | 2019-06-13 |
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