TWI839375B - 一氧化氮釋放第5型磷酸二酯酶抑制劑 - Google Patents

一氧化氮釋放第5型磷酸二酯酶抑制劑 Download PDF

Info

Publication number
TWI839375B
TWI839375B TW108127595A TW108127595A TWI839375B TW I839375 B TWI839375 B TW I839375B TW 108127595 A TW108127595 A TW 108127595A TW 108127595 A TW108127595 A TW 108127595A TW I839375 B TWI839375 B TW I839375B
Authority
TW
Taiwan
Prior art keywords
compound
pyrimidin
nitrooxy
formula
ethyl
Prior art date
Application number
TW108127595A
Other languages
English (en)
Chinese (zh)
Other versions
TW202019491A (zh
Inventor
尼可萊塔 歐米瑞特
斯特法妮婭 布蘭比拉
羅拉 斯朵洛尼
法蘭西斯科 英帕格納蒂耶羅
艾蓮娜 巴斯提亞
Original Assignee
法國商尼可斯股份有限公司
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 法國商尼可斯股份有限公司 filed Critical 法國商尼可斯股份有限公司
Publication of TW202019491A publication Critical patent/TW202019491A/zh
Application granted granted Critical
Publication of TWI839375B publication Critical patent/TWI839375B/zh

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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)
TW108127595A 2018-08-06 2019-08-02 一氧化氮釋放第5型磷酸二酯酶抑制劑 TWI839375B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW202019491A TW202019491A (zh) 2020-06-01
TWI839375B true TWI839375B (zh) 2024-04-21

Family

ID=67539493

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108127595A TWI839375B (zh) 2018-08-06 2019-08-02 一氧化氮釋放第5型磷酸二酯酶抑制劑

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)

* Cited by examiner, † Cited by third party
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017085056A1 (en) * 2015-11-16 2017-05-26 Topadur Pharma Ag 2-phenyl-3,4-dihydropyrrolo[2,1 -f] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

Family Cites Families (23)

* Cited by examiner, † Cited by third party
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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017085056A1 (en) * 2015-11-16 2017-05-26 Topadur Pharma Ag 2-phenyl-3,4-dihydropyrrolo[2,1 -f] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

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
CA3108551A1 (en) 2020-02-13
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
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

Similar Documents

Publication Publication Date Title
TWI839375B (zh) 一氧化氮釋放第5型磷酸二酯酶抑制劑
NL1031976C2 (nl) N-(pyridine-2-yl)sulfonamidederivativen.
US10550102B2 (en) Indane and indoline derivatives and the use thereof as soluble guanylate cyclase activators
US8455484B2 (en) Selected inhibitors of protein tyrosine kinase activity
CN111936139A (zh) 6-氨基异喹啉的单(酸)盐及其用途
ES2969139T3 (es) Composiciones para el tratamiento del glaucoma e hipertensión ocular
CA2837312A1 (en) Metabotropic glutamate receptor 5 allosteric modulators and methods of use thereof
TW201625586A (zh) 環己烯-1-基-吡啶-2-基-1h-吡唑-4-羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途
CN111606852B (zh) 一种一氧化氮供体型Netarsudil衍生物及其制备方法和用途
CN111518028B (zh) 一种一氧化氮供体型ripasudil衍生物及其制备方法和用途
ES2292820T3 (es) 2-(3-sulfonilamino-2-oxopyrrolidin-1-yl)propanamidas como inhibidores del factor xa.
RU2785776C2 (ru) Ингибитор фосфодиэстеразы 5 типа, высвобождающий оксид азота
HK40120357A (zh) 一氧化氮释放第5型磷酸二酯酶抑制剂
HK40049475A (en) Nitric oxide releasing phosphodiesterase type 5 inhibitor
HK40049475B (zh) 一氧化氮释放第5型磷酸二酯酶抑制剂
ES2276307T3 (es) Derivados de 1-fenil-2-oxo-3-sulfonilamino-pirrolidina y compuestos relacionados como inhibidores del factor xa para el tratamiento de enfermedades vasculares agudas.
HK40078239A (en) Compositions for the treatment of glaucoma and ocular hypertension
WO2018224419A1 (en) Nitric oxide donating isomannide derivatives