CA3045491A1 - Integrin antagonists - Google Patents
Integrin antagonists Download PDFInfo
- Publication number
- CA3045491A1 CA3045491A1 CA3045491A CA3045491A CA3045491A1 CA 3045491 A1 CA3045491 A1 CA 3045491A1 CA 3045491 A CA3045491 A CA 3045491A CA 3045491 A CA3045491 A CA 3045491A CA 3045491 A1 CA3045491 A1 CA 3045491A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- unsubstituted
- substituted
- integrin
- alpha
- 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.)
- Abandoned
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- 125000004646 sulfenyl group Chemical group S(*)* 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229960001367 tartaric acid Drugs 0.000 description 1
- 208000022367 tendon sheath fibroma Diseases 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- IOGXOCVLYRDXLW-UHFFFAOYSA-N tert-butyl nitrite Chemical compound CC(C)(C)ON=O IOGXOCVLYRDXLW-UHFFFAOYSA-N 0.000 description 1
- 239000012414 tert-butyl nitrite Substances 0.000 description 1
- MUQNAPSBHXFMHT-UHFFFAOYSA-N tert-butylhydrazine Chemical compound CC(C)(C)NN MUQNAPSBHXFMHT-UHFFFAOYSA-N 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- 230000008467 tissue growth Effects 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- GQHWSLKNULCZGI-UHFFFAOYSA-N trifluoromethoxybenzene Chemical compound FC(F)(F)OC1=CC=CC=C1 GQHWSLKNULCZGI-UHFFFAOYSA-N 0.000 description 1
- MWKJTNBSKNUMFN-UHFFFAOYSA-N trifluoromethyltrimethylsilane Chemical compound C[Si](C)(C)C(F)(F)F MWKJTNBSKNUMFN-UHFFFAOYSA-N 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
- 238000009777 vacuum freeze-drying Methods 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 210000005166 vasculature Anatomy 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 230000007998 vessel formation Effects 0.000 description 1
- 239000000273 veterinary drug Substances 0.000 description 1
- 239000000277 virosome Substances 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 239000000080 wetting agent Substances 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3045491A1 true CA3045491A1 (en) | 2018-07-19 |
Family
ID=62840040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3045491A Abandoned CA3045491A1 (en) | 2016-12-29 | 2017-12-28 | Integrin antagonists |
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 |
|---|---|---|---|---|
| RU2019116820A (ru) | 2016-12-29 | 2021-01-29 | Сент-Луис Юниверсити | Антагонисты интегрина |
| BR112019017929A2 (pt) | 2017-02-28 | 2020-05-19 | Morphic Therapeutic Inc | inibidores de integrina (alfa-v)(beta-6) |
| EP4147698A1 (en) | 2017-02-28 | 2023-03-15 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| ES3019404T3 (en) | 2018-08-29 | 2025-05-20 | Morphic Therapeutic Inc | Integrin inhibitors |
| IL321740A (en) * | 2022-12-27 | 2025-08-01 | Pliant Therapeutics Inc | Alpha-V-beta-8 integrin inhibitors and their uses |
Family Cites Families (16)
| 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 |
| EP1592421A1 (en) | 2002-12-20 | 2005-11-09 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US7115596B2 (en) | 2002-12-20 | 2006-10-03 | Pharmacia Corporation | Thiazole compounds as integrin receptor antagonists derivatives |
| CN104640857B (zh) | 2012-07-18 | 2017-07-04 | 圣路易斯大学 | 作为整合素拮抗剂的β氨基酸衍生物 |
| US8716226B2 (en) * | 2012-07-18 | 2014-05-06 | Saint Louis University | 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists |
| WO2015048819A1 (en) | 2013-09-30 | 2015-04-02 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| ES2925173T3 (es) | 2016-11-08 | 2022-10-14 | Bristol Myers Squibb Co | Acidos propiónicos sustituidos en la posición 3 como inhibidores de la integrina alfa V |
| CA3042714A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Indazole derivatives as a .alpha.v integrin antagonists |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| WO2018089360A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Pyrrole amides as alpha v integrin inhibitors |
| EP3538526B1 (en) | 2016-11-08 | 2024-04-10 | Bristol-Myers Squibb Company | Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors |
| RU2019116820A (ru) | 2016-12-29 | 2021-01-29 | Сент-Луис Юниверсити | Антагонисты интегрина |
| EP4147698A1 (en) | 2017-02-28 | 2023-03-15 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| 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 |
| WO2020009889A1 (en) | 2018-07-03 | 2020-01-09 | Saint Louis University | ALPHAvBETA1 INTEGRIN ANTAGONISTS |
-
2017
- 2017-12-28 RU RU2019116820A patent/RU2019116820A/ru not_active Application Discontinuation
- 2017-12-28 KR KR1020197019720A patent/KR20190100232A/ko not_active Withdrawn
- 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 CA CA3045491A patent/CA3045491A1/en not_active Abandoned
- 2017-12-28 WO PCT/US2017/068801 patent/WO2018132268A1/en not_active Ceased
- 2017-12-28 AU AU2017393297A patent/AU2017393297A1/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 JP JP2019534956A patent/JP2020504120A/ja active Pending
- 2017-12-28 MX MX2019007797A patent/MX2019007797A/es unknown
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018132268A8 (en) | 2019-06-20 |
| WO2018132268A1 (en) | 2018-07-19 |
| RU2019116820A (ru) | 2021-01-29 |
| MX2019007797A (es) | 2019-10-21 |
| EP3562826A4 (en) | 2020-08-26 |
| AU2017393297A1 (en) | 2019-06-13 |
| KR20190100232A (ko) | 2019-08-28 |
| JP2020504120A (ja) | 2020-02-06 |
| IL267686A (en) | 2019-08-29 |
| CN110177787A (zh) | 2019-08-27 |
| CO2019007023A2 (es) | 2019-07-31 |
| PH12019501514A1 (en) | 2020-09-14 |
| US20190345155A1 (en) | 2019-11-14 |
| US11306084B2 (en) | 2022-04-19 |
| EP3562826A1 (en) | 2019-11-06 |
| BR112019012515A2 (pt) | 2019-11-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20220629 |
|
| FZDE | Discontinued |
Effective date: 20220629 |