EA200000702A1 - Пролекарства ингибиторов аспартилпротеаз - Google Patents

Пролекарства ингибиторов аспартилпротеаз

Info

Publication number
EA200000702A1
EA200000702A1 EA200000702A EA200000702A EA200000702A1 EA 200000702 A1 EA200000702 A1 EA 200000702A1 EA 200000702 A EA200000702 A EA 200000702A EA 200000702 A EA200000702 A EA 200000702A EA 200000702 A1 EA200000702 A1 EA 200000702A1
Authority
EA
Eurasian Patent Office
Prior art keywords
prodrugs
relates
inhibitors
pharmaceutical compositions
procaraments
Prior art date
Application number
EA200000702A
Other languages
English (en)
Inventor
Майкл Р. Хейл
Роджер Д. Танг
Кристофер Т. Бейкер
Эндрю Спалтенштейн
Эрик Стивен Ферфайн
Иштван Кальдор
Веслав Мечислав Казмерский
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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 Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of EA200000702A1 publication Critical patent/EA200000702A1/ru

Links

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
    • C07D405/02—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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4172—Imidazole-alkanecarboxylic acids, e.g. histidine
    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7024—Esters of saccharides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings 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
    • C07D307/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings 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
    • C07D317/34—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • C07F9/65844—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a five-membered ring which may be condensed with another ring system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Furan Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

(57) Настоящее изобретение относится к пролекарствам класса сульфонамидов, которые представляют собой ингибиторы аспартилпротеаз. В одном из воплощений данное изобретение относится к новому классу пролекарств, являющихся ингибиторами аспартилпротеаз ВИЧ, характеризующихся хорошей водорастворимостью, высокой биологической доступностью при пероральном применении и легким воспроизведением in vivo активного компонента. Данное изобретение также относится к фармацевтическим композициям, содержащим данные пролекарства. Пролекарство и фармацевтические препараты по данному изобретению особенно хорошо подходят для снижения лекарственной нагрузки и повышения удобства пациентов. Данное изобретение также относится к способам лечения млекопитающих данными пролекарствами и фармацевтическими композициями.Отчет о международном поиске был опубликован 1999.09.10.
EA200000702A 1997-12-24 1998-12-23 Пролекарства ингибиторов аспартилпротеаз EA200000702A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6888997P 1997-12-24 1997-12-24
PCT/US1998/027424 WO1999033793A2 (en) 1997-12-24 1998-12-23 Prodrugs of aspartyl protease inhibitors

Publications (1)

Publication Number Publication Date
EA200000702A1 true EA200000702A1 (ru) 2000-12-25

Family

ID=22085350

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000702A EA200000702A1 (ru) 1997-12-24 1998-12-23 Пролекарства ингибиторов аспартилпротеаз

Country Status (21)

Country Link
US (2) US20020082249A1 (ru)
EP (1) EP1042280A2 (ru)
JP (1) JP2001527062A (ru)
KR (1) KR20010033595A (ru)
CN (1) CN1110492C (ru)
AP (1) AP2000001856A0 (ru)
AU (1) AU2092599A (ru)
BR (1) BR9814484A (ru)
CA (1) CA2316218A1 (ru)
EA (1) EA200000702A1 (ru)
EE (1) EE200000386A (ru)
HR (1) HRP20000499A2 (ru)
HU (1) HUP0101598A3 (ru)
ID (1) ID25551A (ru)
IL (1) IL136940A0 (ru)
IS (1) IS5547A (ru)
NO (1) NO20003332L (ru)
PL (1) PL341762A1 (ru)
SK (1) SK9672000A3 (ru)
TR (1) TR200002402T2 (ru)
WO (1) WO1999033793A2 (ru)

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
GB9815567D0 (en) * 1998-07-18 1998-09-16 Glaxo Group Ltd Antiviral compound
HU229224B1 (en) * 2001-02-14 2013-09-30 Tibotec Pharmaceuticals Ltd Little Island 2-(substituted-amino)-benzothiazole sulfonamide compounds having broadspectrum hiv protease inhibitor activity and medicaments containing them
OA12464A (en) 2001-04-09 2006-05-24 Tibotec Pharm Ltd Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide HIV protease inhibitors.
JP2004534017A (ja) * 2001-04-27 2004-11-11 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｂａｃｅのインヒビター
DK1387842T3 (da) 2001-05-11 2009-08-10 Tibotec Pharm Ltd Bredspektrede 2-amino-benzoxazolsulfonamid-HIV-protease-inhibitorer
MY138657A (en) 2001-12-21 2009-07-31 Tibotec Pharm Ltd broadspectrum heterocyclic substituted phenyl containing sulfonamide hiv protease inhibitors
MY142238A (en) 2002-03-12 2010-11-15 Tibotec Pharm Ltd Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors
KR100987815B1 (ko) * 2002-04-26 2010-10-18 길리애드 사이언시즈, 인코포레이티드 Ｈｉｖ 프로테아제 억제제 화합물의 포스포네이트유사체의 세포 축적
JP4674084B2 (ja) 2002-05-17 2011-04-20 テイボテク・フアーマシユーチカルズ・リミテツド 広域スペクトルの置換ベンズイソキサゾールスルホンアミドｈｉｖプロテアーゼ阻害剤
NZ538714A (en) 2002-08-14 2007-03-30 Tibotec Pharm Ltd Broadspectrum substituted oxindole sulfonamide HIV protease inhibitors
DE10259245A1 (de) 2002-12-17 2004-07-01 Merck Patent Gmbh Derivate des Asimadolins mit kovalent gebundenen Säuren
US6632816B1 (en) * 2002-12-23 2003-10-14 Pharmacor Inc. Aromatic derivatives as HIV aspartyl protease inhibitors
UA83881C2 (en) 2003-12-18 2008-08-26 Янссен Фармацевтика Н.В. Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents
US7388008B2 (en) 2004-08-02 2008-06-17 Ambrilia Biopharma Inc. Lysine based compounds
WO2006024489A2 (en) 2004-08-30 2006-03-09 Interstitial Therapeutics Methods and compositions for the treatment of cell proliferation
BRPI0516915A (pt) 2004-12-01 2008-03-11 Devgen Nv derivados de tiazol substituìdos por 5-carboxamido que interagem com canais de ìons, particularmante com canais de ìons da famìlia kv
NI200700147A (es) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv Derivados de quinazolina inhibidores de cinasas dirigidos a multip
EP1941799A3 (en) 2004-12-17 2008-09-17 Devgen NV Nematicidal compositions
US8003627B2 (en) 2005-10-21 2011-08-23 Universiteit Antwerpen Urokinase inhibitors
TWI432438B (zh) 2005-11-28 2014-04-01 Tibotec Pharm Ltd 作為ｈｉｖ蛋白酶抑制劑之經取代的胺基苯基磺醯胺化合物及衍生物
TWI385173B (zh) 2005-11-28 2013-02-11 Tibotec Pharm Ltd 作為ｈｉｖ蛋白酶抑制劑之經取代的胺基苯基磺醯胺化合物
CN101405293B (zh) 2005-11-30 2013-03-13 中裕新药股份有限公司 天冬氨酰基蛋白酶抑制剂基于赖氨酸的前体药物及其制备方法
JP2009542778A (ja) 2006-07-13 2009-12-03 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｍｔｋｉキナゾリン誘導体
EP2289564A3 (en) 2006-09-08 2012-11-14 Piramal Imaging SA Derivatives of aniline as precursors for F18-labeling
JP5401652B2 (ja) 2006-09-21 2014-01-29 タイメッド バイオロジクス インコーポレイテッド プロテアーゼ阻害剤
DK2185562T3 (en) 2007-07-27 2016-02-22 Janssen Pharmaceutica Nv PYRROLOPYRIMIDINES SUITABLE FOR TREATING PROLIFERATIVE DISEASES
EP2053033A1 (en) 2007-10-26 2009-04-29 Bayer Schering Pharma AG Compounds for use in imaging, diagnosing and/or treatment of diseases of the central nervous system or of tumors
EP2100900A1 (en) 2008-03-07 2009-09-16 Universitätsspital Basel Bombesin analog peptide antagonist conjugates
JP5480824B2 (ja) 2008-03-10 2014-04-23 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｐｌｋキナーゼ阻害剤としての４−アリール−２−アニリノ−ピリミジン
EP2116236A1 (en) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
WO2011061295A1 (en) 2009-11-19 2011-05-26 Blue Medical Devices Bv Narrow profile composition-releasing expandable medical balloon catheter
WO2011141515A1 (en) 2010-05-14 2011-11-17 Bayer Pharma Aktiengesellschaft Diagnostic agents for amyloid beta imaging
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
GB201019043D0 (en) 2010-11-10 2010-12-22 Protea Biopharma N V Use of 2',5'-oligoadenylate derivative compounds
CN112961855A (zh) 2011-06-21 2021-06-15 阿尔尼拉姆医药品有限公司 血管生成素样3(ANGPTL3)iRNA组合物及其使用方法
WO2012178033A2 (en) 2011-06-23 2012-12-27 Alnylam Pharmaceuticals, Inc. Serpina1 sirnas: compositions of matter and methods of treatment
US9127274B2 (en) 2012-04-26 2015-09-08 Alnylam Pharmaceuticals, Inc. Serpinc1 iRNA compositions and methods of use thereof
EP2700396A3 (en) 2012-06-20 2015-04-29 Sylphar Nv Strip for the delivery of oral care compositions
US9877981B2 (en) 2012-10-09 2018-01-30 President And Fellows Of Harvard College NAD biosynthesis and precursors for the treatment and prevention of cancer and proliferation
HUE035887T2 (en) 2012-12-05 2018-05-28 Alnylam Pharmaceuticals Inc PCSK9 iRNA preparations and methods for their use
CN114015692A (zh) 2013-03-14 2022-02-08 阿尔尼拉姆医药品有限公司 补体组分C5 iRNA组合物及其使用方法
CN105408481B (zh) 2013-05-22 2021-03-30 阿尔尼拉姆医药品有限公司 SERPINA1 iRNA组合物及其使用方法
TW202342750A (zh) 2013-05-22 2023-11-01 美商阿尼拉製藥公司 ＴＭＰＲＳＳ６ ｉＲＮＡ組成物及其使用方法
CN105814205B (zh) 2013-12-12 2019-11-19 阿尔尼拉姆医药品有限公司 补体成分iRNA组合物及其使用方法
WO2015123264A1 (en) 2014-02-11 2015-08-20 Alnylam Pharmaceuticals, Inc. Ketohexokinase (khk) irna compositions and methods of use thereof
WO2015175510A1 (en) 2014-05-12 2015-11-19 Alnylam Pharmaceuticals, Inc. Methods and compositions for treating a serpinc1-associated disorder
EP3146049B1 (en) 2014-05-22 2020-02-26 Alnylam Pharmaceuticals, Inc. Angiotensinogen (agt) irna compositions and methods of use thereof
EP3180003B1 (en) 2014-07-01 2022-01-12 The Regents of the University of California Pkc-epsilon inhibitors
WO2016040589A1 (en) 2014-09-12 2016-03-17 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting complement component c5 and methods of use thereof
EP3207138B1 (en) 2014-10-17 2020-07-15 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting aminolevulinic acid synthase-1 (alas1) and uses thereof
WO2016069694A2 (en) 2014-10-30 2016-05-06 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting serpinc1 (at3) and methods of use thereof
WO2016081444A1 (en) 2014-11-17 2016-05-26 Alnylam Pharmaceuticals, Inc. Apolipoprotein c3 (apoc3) irna compositions and methods of use thereof
WO2016083490A1 (en) 2014-11-27 2016-06-02 Remynd Nv Compounds for the treatment of amyloid-associated diseases
WO2016130806A2 (en) 2015-02-13 2016-08-18 Alnylam Pharmaceuticals, Inc. Patatin-like phospholipase domain containing 3 (pnpla3) irna compositions and methods of use thereof
AU2016247922B2 (en) 2015-04-13 2022-04-28 Alnylam Pharmaceuticals, Inc. Angiopoietin-like 3 (ANGPTL3) iRNA compositions and methods of use thereof
DK3288637T3 (da) 2015-04-28 2022-10-17 Newsouth Innovations Pty Ltd Målretning af nad+ til behandling af kemoterapi- og radioterapi-induceret, kognitiv funktionsnedsættelse, neuropatier og inaktivitet
EP3292201A2 (en) 2015-05-06 2018-03-14 Alnylam Pharmaceuticals, Inc. Factor xii (hageman factor) (f12), kallikrein b, plasma (fletcher factor) 1 (klkb1), and kininogen 1 (kng1) irna compositions and methods of use thereof
WO2016201301A1 (en) 2015-06-12 2016-12-15 Alnylam Pharmaceuticals, Inc. Complement component c5 irna compositions and methods of use thereof
EP3310918B1 (en) 2015-06-18 2020-08-05 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting hydroxyacid oxidase (glycolate oxidase, hao1) and methods of use thereof
WO2017048620A1 (en) 2015-09-14 2017-03-23 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting patatin-like phospholipase domain containing 3 (pnpla3) and methods of use thereof
TWI836281B (zh) 2015-12-07 2024-03-21 美商健贊公司 治療ｓｅｒｐｉｎｃ１相關疾患之方法及組成物
JP2018536689A (ja) 2015-12-10 2018-12-13 アルナイラム ファーマシューティカルズ， インコーポレイテッドＡｌｎｙｌａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． ステロール調節エレメント結合タンパク質（ＳＲＥＢＰ）シャペロン（ＳＣＡＰ）ｉＲＮＡ組成物およびその使用方法
US20190256845A1 (en) 2016-06-10 2019-08-22 Alnylam Pharmaceuticals, Inc. COMPLEMENT COMPONENT C5 iRNA COMPOSITIONS AND METHODS OF USE THEREOF FOR TREATING PAROXYSMAL NOCTURNAL HEMOGLOBINURIA (PNH)
TWI788312B (zh) 2016-11-23 2023-01-01 美商阿尼拉製藥公司 絲胺酸蛋白酶抑制因子Ａ１ ｉＲＮＡ組成物及其使用方法
KR20230166146A (ko) 2016-12-16 2023-12-06 알닐람 파마슈티칼스 인코포레이티드 트랜스티레틴(TTR) iRNA 조성물을 사용하여 TTR-관련 질병을 치료하거나 예방하는 방법
EA201992397A1 (ru) 2017-05-11 2020-03-16 Реминд Н.В. Соединения для лечения эпилепсии, нейродегенеративных нарушений и других нарушений цнс
US11866701B2 (en) 2017-11-01 2024-01-09 Alnylam Pharmaceuticals, Inc. Complement component C3 iRNA compositions and methods of use thereof
US11492623B2 (en) 2018-08-13 2022-11-08 Alnylam Pharmaceuticals, Inc. Hepatitis B virus (HBV) dsRNA agent compositions and methods of use thereof
US20220079971A1 (en) 2019-01-16 2022-03-17 Genzyme Corporation SERPINC1 iRNA Compositions and Methods of Use Thereof
WO2021154941A1 (en) 2020-01-31 2021-08-05 Alnylam Pharmaceuticals, Inc. Complement component c5 irna compositions for use in the treatment of amyotrophic lateral sclerosis (als)
EP4110777A1 (en) 2020-02-24 2023-01-04 Katholieke Universiteit Leuven, K.U.Leuven R&D Pyrrolopyridine and imidazopyridine antiviral compounds
JP2024500543A (ja) 2020-12-22 2024-01-09 ルクセンブルク インスティテュート オブ ヘルス（エルアイエイチ） がん及び循環器疾患の処置のための選択的ａｃｋｒ３調節物質としてのコノリジンアナログ
EP4301369A1 (en) 2021-03-04 2024-01-10 Universiteit Antwerpen Quinazolin-4-one and thieno[2,3-d]pyrimidin-4-one inhibitors of erbb4 (her4) for use in the treatment of cancer
AU2022286613A1 (en) 2021-05-31 2023-11-23 Telix Pharmaceuticals (Innovations) Pty Ltd Improved prostate-specific membrane antigen targeting radiopharmaceuticals and uses thereof
WO2023021132A1 (en) 2021-08-18 2023-02-23 Katholieke Universiteit Leuven 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
WO2023046900A1 (en) 2021-09-23 2023-03-30 Katholieke Universiteit Leuven Ribonucleoside analogues against -sars-cov-2
WO2023241799A1 (en) 2022-06-15 2023-12-21 Université Libre de Bruxelles Flavanols for use in the treatment of retroviral infections
WO2024062043A1 (en) 2022-09-21 2024-03-28 Universiteit Antwerpen Substituted phenothiazines as ferroptosis inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
AU7669794A (en) * 1993-08-24 1995-03-21 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease

Also Published As

Publication number Publication date
US20030144217A1 (en) 2003-07-31
WO1999033793A3 (en) 1999-09-10
SK9672000A3 (en) 2001-04-09
IS5547A (is) 2000-06-22
JP2001527062A (ja) 2001-12-25
BR9814484A (pt) 2000-10-10
CN1110492C (zh) 2003-06-04
ID25551A (id) 2000-10-12
WO1999033793A2 (en) 1999-07-08
PL341762A1 (en) 2001-05-07
NO20003332D0 (no) 2000-06-26
EP1042280A2 (en) 2000-10-11
EE200000386A (et) 2001-12-17
US20020082249A1 (en) 2002-06-27
AP2000001856A0 (en) 2000-09-30
HRP20000499A2 (en) 2001-04-30
TR200002402T2 (tr) 2001-01-22
CA2316218A1 (en) 1999-07-08
HUP0101598A3 (en) 2002-08-28
AU2092599A (en) 1999-07-19
IL136940A0 (en) 2001-06-14
KR20010033595A (ko) 2001-04-25
HUP0101598A2 (hu) 2002-04-29
CN1284072A (zh) 2001-02-14
NO20003332L (no) 2000-08-18

Similar Documents

Publication Publication Date Title
EA200000702A1 (ru) Пролекарства ингибиторов аспартилпротеаз
EA200000703A1 (ru) Сульфонамидные производные в качестве пролекарств, ингибиторов аспартилпротеаз
EA200300065A1 (ru) Окисленные сложные эфиры 4-йодфениламинобензгидроксамовых кислот
EA200000871A1 (ru) Ингибиторы фосфолипазных ферментов
EA200100872A1 (ru) Композиция валдекоксиба
EA200201271A1 (ru) Ингибиторы 11-бета-гидроксистероиддегидрогеназы типа 1
EA200200619A1 (ru) Непептидильные ингибиторы vla-4-зависимого связывания клеток, применяемые при лечении воспалительных, аутоимунных и респираторных заболеваний
ATE554750T1 (de) Hydrophobe pharmazeutische wirkstoffe enthaltende zubereitungen
EA200100971A1 (ru) Новые соединения и композиции в качестве ингибиторов протеазы
PT951474E (pt) Novos derivados da ciclosporina sua preparacao e composicoes farmaceuticas que os contem
EA200200938A1 (ru) Фармацевтические композиции, содержащие производные азетидина, новые производные азетидина и их получение
RU95101048A (ru) Производные пролинамида, фармкомпозиция на их основе
WO1999033792A3 (en) Prodrugs os aspartyl protease inhibitors
EA199901031A1 (ru) Производные бензимидазола
CA2217737A1 (en) Thf-containing sulfonamide inhibitors of aspartyl protease
AP9600827A0 (en) Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease.
YU23599A (sh) Stabilizovani antihistaminski sirup
CO4940450A1 (es) Formulaciones farmaceuticas que contienen voriconazol
DE69828496D1 (de) Hydrophile binäre systeme zur verabreichung von cyclosporin
DK0996429T3 (da) Faste opløsninger og faste dispersioner i vand tungtopløselige lægemidler
ATE277929T1 (de) Immunsuppressive wirkungen von pteridinderivaten
RU93004907A (ru) Производные гидроксамовой кислоты и n-гидроксимочевины. способ их получения фармацевтическая композиция и способ лечения
BR9811099A (pt) Inibidores de urocinase
EA200200713A1 (ru) Сульфонамиды и их производные, модулирующие активность эндотелина
ATE147981T1 (de) Verabreichung von lamotrigin zur behandlung von neuro-aids