CN114025759A - 用于治疗眼病的化合物和方法 - Google Patents
用于治疗眼病的化合物和方法 Download PDFInfo
- Publication number
- CN114025759A CN114025759A CN202080044807.9A CN202080044807A CN114025759A CN 114025759 A CN114025759 A CN 114025759A CN 202080044807 A CN202080044807 A CN 202080044807A CN 114025759 A CN114025759 A CN 114025759A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- compound
- optionally substituted
- heteroalkyl
- group
- 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
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962835963P | 2019-04-18 | 2019-04-18 | |
| US62/835,963 | 2019-04-18 | ||
| PCT/IB2020/000288 WO2020212755A1 (en) | 2019-04-18 | 2020-04-16 | Compounds and methods for the treatment of ocular disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN114025759A true CN114025759A (zh) | 2022-02-08 |
Family
ID=72832983
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080044807.9A Pending CN114025759A (zh) | 2019-04-18 | 2020-04-16 | 用于治疗眼病的化合物和方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US10875845B2 (https=) |
| EP (1) | EP3955926A4 (https=) |
| JP (1) | JP7700045B2 (https=) |
| KR (1) | KR20220003555A (https=) |
| CN (1) | CN114025759A (https=) |
| IL (1) | IL287264A (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116635032A (zh) * | 2020-10-21 | 2023-08-22 | 阿祖拉眼科有限公司 | 用于治疗眼部病症的化合物和方法 |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7700045B2 (ja) * | 2019-04-18 | 2025-06-30 | アズーラ オフサルミックス エルティーディー. | 眼障害を処置するための化合物および方法 |
| IL302175A (en) * | 2020-10-21 | 2023-06-01 | Azura Ophthalmics Ltd | Compounds and methods for the treatment of ocular disorders |
| US11459351B1 (en) | 2021-04-05 | 2022-10-04 | Azura Ophthalmics Ltd. | Compounds and methods for the treatment of ocular disorders |
| EP4419502A4 (en) * | 2021-10-20 | 2025-10-29 | Azura Ophthalmics Ltd | COMPOUNDS AND METHODS FOR THE TREATMENT OF SKIN AND OCULAR DISORDERS |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102065694A (zh) * | 2008-04-15 | 2011-05-18 | 萨可德公司 | 用于局部治疗免疫相关疾病的雾化的lfa-1拮抗剂 |
| CN104797574A (zh) * | 2012-07-25 | 2015-07-22 | 原生质生物科学股份有限公司 | Lfa-1抑制剂及其多晶型物 |
| CN104955453A (zh) * | 2012-12-19 | 2015-09-30 | 原生质生物科学股份有限公司 | Lfa-1抑制剂制剂 |
| WO2019053607A1 (en) * | 2017-09-18 | 2019-03-21 | Glenmark Pharmaceuticals Limited | PROCESS FOR PREPARING LIFITEGRAST |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6334997B1 (en) | 1994-03-25 | 2002-01-01 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
| ES2293638T3 (es) | 1994-03-25 | 2008-03-16 | Isotechnika, Inc. | Mejora de la eficacia de farmacos por deuteracion. |
| US7056893B2 (en) | 1999-03-31 | 2006-06-06 | Insite Vision, Inc. | Topical treatment for prevention of ocular infections |
| US6239113B1 (en) | 1999-03-31 | 2001-05-29 | Insite Vision, Incorporated | Topical treatment or prevention of ocular infections |
| EP1483579A4 (en) | 2002-02-15 | 2006-07-12 | Merckle Gmbh | CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, PROCESS FOR THEIR MANUFACTURE AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF |
| CA2544678C (en) | 2003-11-05 | 2013-12-31 | Sunesis Pharmaceuticals, Inc. | Modulators of cellular adhesion |
| DK2444079T3 (en) | 2005-05-17 | 2017-01-30 | Sarcode Bioscience Inc | Compositions and Methods for the Treatment of Eye Diseases |
| DE102005062987A1 (de) | 2005-12-28 | 2007-07-05 | Grünenthal GmbH | Substituierte Propiolsäureamide und ihre Verwendung zur Herstellung von Arzneimitteln |
| WO2009128934A1 (en) * | 2008-04-15 | 2009-10-22 | Sarcode Corporation | Topical lfa-1 antagonists for use in localized treatment of immune related disorders |
| WO2009139817A2 (en) | 2008-04-15 | 2009-11-19 | Sarcode Corporation | Crystalline pharmaceutical and methods of preparation and use thereof |
| WO2011050175A1 (en) | 2009-10-21 | 2011-04-28 | Sarcode Corporation | Crystalline pharmaceutical and methods of preparation and use thereof |
| US9463201B2 (en) | 2014-10-19 | 2016-10-11 | M.G. Therapeutics Ltd | Compositions and methods for the treatment of meibomian gland dysfunction |
| JP2019513775A (ja) | 2016-04-19 | 2019-05-30 | アズーラ オフサルミックス エルティーディー. | 角化症の処置のための組成物 |
| WO2018161039A1 (en) | 2017-03-03 | 2018-09-07 | Synovo Gmbh | Novel anti-infective and anti-inflammatory compounds |
| EP3600272A4 (en) | 2017-03-29 | 2021-01-13 | Azura Ophthalmics Ltd. | MEANS OF INCREASING LIPID SECRETION OF THE MEIBOMAN GLAND |
| EP3955937A4 (en) | 2019-04-18 | 2023-01-18 | Azura Ophthalmics Ltd. | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF EYE DISEASES |
| WO2020212755A1 (en) | 2019-04-18 | 2020-10-22 | Azura Ophthalmics Ltd. | Compounds and methods for the treatment of ocular disorders |
| JP7700045B2 (ja) | 2019-04-18 | 2025-06-30 | アズーラ オフサルミックス エルティーディー. | 眼障害を処置するための化合物および方法 |
| IL302173A (en) | 2020-10-21 | 2023-06-01 | Azura Ophthalmics Ltd | Compounds and methods for the treatment of ocular disorders |
| US11459351B1 (en) | 2021-04-05 | 2022-10-04 | Azura Ophthalmics Ltd. | Compounds and methods for the treatment of ocular disorders |
-
2020
- 2020-04-16 JP JP2021559917A patent/JP7700045B2/ja active Active
- 2020-04-16 KR KR1020217037591A patent/KR20220003555A/ko not_active Ceased
- 2020-04-16 EP EP20791787.3A patent/EP3955926A4/en active Pending
- 2020-04-16 CN CN202080044807.9A patent/CN114025759A/zh active Pending
- 2020-06-17 US US16/904,036 patent/US10875845B2/en active Active
- 2020-12-04 US US17/112,371 patent/US11634411B2/en active Active
-
2021
- 2021-10-14 IL IL287264A patent/IL287264A/en unknown
-
2023
- 2023-03-08 US US18/119,248 patent/US20230357207A1/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102065694A (zh) * | 2008-04-15 | 2011-05-18 | 萨可德公司 | 用于局部治疗免疫相关疾病的雾化的lfa-1拮抗剂 |
| CN104797574A (zh) * | 2012-07-25 | 2015-07-22 | 原生质生物科学股份有限公司 | Lfa-1抑制剂及其多晶型物 |
| CN104955453A (zh) * | 2012-12-19 | 2015-09-30 | 原生质生物科学股份有限公司 | Lfa-1抑制剂制剂 |
| WO2019053607A1 (en) * | 2017-09-18 | 2019-03-21 | Glenmark Pharmaceuticals Limited | PROCESS FOR PREPARING LIFITEGRAST |
Non-Patent Citations (2)
| Title |
|---|
| CHARLES P. SEMBA ET AL.: "A Phase 2 Randomized, Double-Masked, Placebo-Controlled Study of a Novel Integrin Antagonist (SAR 1118) for the Treatment of Dry Eye", 《AMERICAN JOURNAL OF OPHTHALMOLOGY》, vol. 153, no. 6, pages 1050 - 1060 * |
| MIN ZHONG ET AL.: "Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye", 《ACS MED. CHEM. LETT.》, vol. 3, no. 3, pages 203 - 206, XP055115083, DOI: 10.1021/ml2002482 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116635032A (zh) * | 2020-10-21 | 2023-08-22 | 阿祖拉眼科有限公司 | 用于治疗眼部病症的化合物和方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP7700045B2 (ja) | 2025-06-30 |
| KR20220003555A (ko) | 2022-01-10 |
| US20210107899A1 (en) | 2021-04-15 |
| EP3955926A4 (en) | 2022-11-30 |
| US11634411B2 (en) | 2023-04-25 |
| US20200331896A1 (en) | 2020-10-22 |
| EP3955926A1 (en) | 2022-02-23 |
| IL287264A (en) | 2021-12-01 |
| US10875845B2 (en) | 2020-12-29 |
| US20230357207A1 (en) | 2023-11-09 |
| JP2022530322A (ja) | 2022-06-29 |
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| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 40068671 Country of ref document: HK |
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| RJ01 | Rejection of invention patent application after publication |
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