CA3108551A1 - Nitric oxide releasing phosphodiesterase type 5 inhibitor - Google Patents
Nitric oxide releasing phosphodiesterase type 5 inhibitor Download PDFInfo
- Publication number
- CA3108551A1 CA3108551A1 CA3108551A CA3108551A CA3108551A1 CA 3108551 A1 CA3108551 A1 CA 3108551A1 CA 3108551 A CA3108551 A CA 3108551A CA 3108551 A CA3108551 A CA 3108551A CA 3108551 A1 CA3108551 A1 CA 3108551A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- pyrimidin
- formula
- nitrooxy
- ethyl
- 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
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18187482.7 | 2018-08-06 | ||
| EP18187482 | 2018-08-06 | ||
| EP18210147.7 | 2018-12-04 | ||
| EP18210147 | 2018-12-04 | ||
| PCT/EP2019/070597 WO2020030489A1 (en) | 2018-08-06 | 2019-07-31 | Nitric oxide releasing phosphodiesterase type 5 inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3108551A1 true CA3108551A1 (en) | 2020-02-13 |
Family
ID=67539493
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3108551A Pending CA3108551A1 (en) | 2018-08-06 | 2019-07-31 | Nitric oxide releasing phosphodiesterase type 5 inhibitor |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11980618B2 (https=) |
| EP (1) | EP3833395A1 (https=) |
| JP (2) | JP7596257B2 (https=) |
| KR (1) | KR102836746B1 (https=) |
| CN (2) | CN119350347A (https=) |
| AU (1) | AU2019319004B2 (https=) |
| BR (1) | BR112021001950A2 (https=) |
| CA (1) | CA3108551A1 (https=) |
| MX (2) | MX2021001503A (https=) |
| TW (1) | TWI839375B (https=) |
| WO (1) | WO2020030489A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7708771B2 (ja) * | 2020-02-05 | 2025-07-15 | ニコックス エス.エー. | 緑内障及び高眼圧症の処置のための組成物 |
| CN111217834B (zh) * | 2020-02-21 | 2021-10-26 | 维眸生物科技(上海)有限公司 | Rock激酶抑制剂的硝基氧衍生物 |
| WO2022022669A1 (en) * | 2020-07-30 | 2022-02-03 | Biofront Therapeutics (Beijing) Co., Ltd. | Dual-functional compounds and methods of use |
| KR102731727B1 (ko) * | 2020-07-30 | 2024-11-20 | 바이오프런트 쎄라퓨틱스 (베이징) 컴퍼니 리미티드 | 이중-기능성 화합물 및 이의 사용 방법 |
| CN116456963A (zh) * | 2020-11-02 | 2023-07-18 | 尼科斯股份有限公司 | 用于治疗干性年龄相关性黄斑变性、地图状萎缩和青光眼相关性神经变性的no-pde5抑制剂 |
| UY39509A (es) * | 2020-11-09 | 2022-01-31 | Ildong Pharmaceutical Co Ltd | Compuestos inhibidores de la pde-5 y/o la pde-6 donantes de óxido de nitrógeno, y usos de estos |
| WO2023005180A1 (en) * | 2021-07-30 | 2023-02-02 | Biofront Therapeutics (Beijing) Co., Ltd. | Dual-functional compounds and methods of use |
| JP2024541626A (ja) | 2021-12-02 | 2024-11-08 | ニコックス エス.エー. | 一酸化窒素放出ホスホジエステラーゼ5阻害剤を含有する眼科用医薬組成物及びその製造方法 |
| EP4233867B1 (en) | 2022-02-24 | 2025-09-03 | Nicox SA | Pde5 inhibitor for use in the treatment of anterior ischemic optic neuropathy |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60149521A (ja) | 1984-01-18 | 1985-08-07 | Eisai Co Ltd | 高眼圧・緑内障治療・予防用点眼剤 |
| US4975428A (en) | 1988-05-31 | 1990-12-04 | Iolab Corporation | Treatment of glaucoma using phosphodiesterase inhibitors |
| GB9013750D0 (en) | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
| IL137429A0 (en) | 1999-07-28 | 2001-07-24 | Pfizer Prod Inc | Methods and compsitions for treating diseases and conditions of the eye |
| EP1219609B1 (en) | 1999-09-16 | 2007-04-04 | Tanabe Seiyaku Co., Ltd. | Aromatic nitrogenous six-membered ring compounds |
| KR100358083B1 (ko) * | 2000-02-17 | 2002-10-25 | 에스케이케미칼주식회사 | 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도 |
| US20020168424A1 (en) | 2002-07-31 | 2002-11-14 | Dr. Mohsen Shahinpoor | Nitric oxide (NO) donor+cGMP-PDE5 inhibitor as a topical drug for glaucoma |
| DE102005001989A1 (de) * | 2005-01-15 | 2006-07-20 | Bayer Healthcare Ag | Intravenöse Formulierungen von PDE-Inhibitoren |
| WO2008075152A1 (en) * | 2006-12-15 | 2008-06-26 | Pfizer Products Inc. | 1- [4- (sulfonyl) -phenyl] -5- (benzyl) -ih-i, 2, 4-triazol derivatives as inhibitors of carbonic anhydrase for treating glaucoma or ocular hypertension |
| US7993616B2 (en) | 2007-09-19 | 2011-08-09 | C-Quest Technologies LLC | Methods and devices for reducing hazardous air pollutants |
| ES2393049T3 (es) | 2008-02-07 | 2012-12-18 | Nicox S.A. | Compuestos donantes de óxido nítrico |
| EP2398761A4 (en) * | 2009-02-18 | 2015-11-04 | Bezwada Biomedical Llc | CONTROLLED RELEASE OF NITRIC OXIDE AND MEDICINES FROM FUNCTIONALIZED MACROMERS AND OLIGOMERS |
| CN102498088A (zh) * | 2009-09-15 | 2012-06-13 | 帝斯曼知识产权资产管理有限公司 | 硝基氧基酯及其制备和用途 |
| AU2010330813B2 (en) * | 2009-12-18 | 2016-04-28 | Exodos Life Sciences Limited Partnership | Methods and compositions for treating peripheral vascular disease |
| US9446015B2 (en) | 2012-10-23 | 2016-09-20 | Nicox Science Ireland | Quinone based nitric oxide donating compounds for ophthalmic use |
| EP2826491A1 (en) * | 2013-07-15 | 2015-01-21 | Nicox Science Ireland | Ophthalmic compositions containing a nitric oxide donor |
| TW201625584A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| ES2632808T3 (es) | 2014-09-04 | 2017-09-15 | Nicox Science Ireland | Compuestos de carnosina donadores de óxido nítrico |
| US10610509B2 (en) | 2014-11-19 | 2020-04-07 | Nicox S.A. | Combinations of prostaglandins and nitric oxide donors |
| US10280138B2 (en) * | 2015-03-31 | 2019-05-07 | Nicox S.A. | Nitric oxide donating derivatives of fluprostenol |
| US10047047B2 (en) | 2015-03-31 | 2018-08-14 | Nicox S.A. | Nitric oxide donating derivatives of latanoprost free acid |
| EP3088388A1 (en) * | 2015-04-30 | 2016-11-02 | NicOx S.A. | Nitric oxide donating derivatives of prostaglandins |
| PL3377495T3 (pl) * | 2015-11-16 | 2022-05-16 | Topadur Pharma Ag | Pochodne 2-fenylo-3,4-dihydropirolo[2,1-f] [1,2,4]triazynonu jako inhibitory fosfodiesterazy i ich zastosowania |
| KR102670626B1 (ko) | 2017-05-22 | 2024-05-29 | 토파두르 파마 아게 | 가용성 구아닐레이트 사이클라제 활성제 및 포스포디에스테라제 억제제의 신규한 이중 작용 방식 및 이의 용도 |
-
2019
- 2019-07-31 JP JP2021506326A patent/JP7596257B2/ja active Active
- 2019-07-31 CN CN202411482883.4A patent/CN119350347A/zh active Pending
- 2019-07-31 KR KR1020217006735A patent/KR102836746B1/ko active Active
- 2019-07-31 CN CN201980052271.2A patent/CN112566670B/zh active Active
- 2019-07-31 AU AU2019319004A patent/AU2019319004B2/en active Active
- 2019-07-31 BR BR112021001950-2A patent/BR112021001950A2/pt unknown
- 2019-07-31 US US17/265,134 patent/US11980618B2/en active Active
- 2019-07-31 MX MX2021001503A patent/MX2021001503A/es unknown
- 2019-07-31 EP EP19749305.9A patent/EP3833395A1/en active Pending
- 2019-07-31 WO PCT/EP2019/070597 patent/WO2020030489A1/en not_active Ceased
- 2019-07-31 CA CA3108551A patent/CA3108551A1/en active Pending
- 2019-08-02 TW TW108127595A patent/TWI839375B/zh active
-
2021
- 2021-02-05 MX MX2023012941A patent/MX2023012941A/es unknown
-
2024
- 2024-03-22 US US18/614,143 patent/US20240245684A1/en active Pending
- 2024-08-01 JP JP2024125823A patent/JP2024150732A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2024150732A (ja) | 2024-10-23 |
| WO2020030489A1 (en) | 2020-02-13 |
| CN112566670B (zh) | 2024-11-12 |
| US20210322413A1 (en) | 2021-10-21 |
| JP7596257B2 (ja) | 2024-12-09 |
| EP3833395A1 (en) | 2021-06-16 |
| US20240245684A1 (en) | 2024-07-25 |
| KR102836746B1 (ko) | 2025-07-21 |
| KR20210041596A (ko) | 2021-04-15 |
| US11980618B2 (en) | 2024-05-14 |
| MX2021001503A (es) | 2021-04-28 |
| BR112021001950A2 (pt) | 2021-04-27 |
| TW202019491A (zh) | 2020-06-01 |
| AU2019319004A1 (en) | 2021-03-25 |
| TWI839375B (zh) | 2024-04-21 |
| JP2021533152A (ja) | 2021-12-02 |
| CN119350347A (zh) | 2025-01-24 |
| MX2023012941A (es) | 2023-11-13 |
| AU2019319004B2 (en) | 2025-04-24 |
| CN112566670A (zh) | 2021-03-26 |
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