ZA200800314B - Phosphoramidate alkylator prodrugs - Google Patents

Phosphoramidate alkylator prodrugs

Info

Publication number
ZA200800314B
ZA200800314B ZA200800314A ZA200800314A ZA200800314B ZA 200800314 B ZA200800314 B ZA 200800314B ZA 200800314 A ZA200800314 A ZA 200800314A ZA 200800314 A ZA200800314 A ZA 200800314A ZA 200800314 B ZA200800314 B ZA 200800314B
Authority
ZA
South Africa
Prior art keywords
phosphoramidate alkylator
alkylator prodrugs
prodrugs
phosphoramidate
alkylator
Prior art date
Application number
ZA200800314A
Other languages
English (en)
Inventor
Matteucci Mark
Duan Jian-Xin
Jiao Hailong
Kaizerman Jacob
Ammons Steve
Original Assignee
Threshold Pharmaceuticals Inc
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 Threshold Pharmaceuticals Inc filed Critical Threshold Pharmaceuticals Inc
Publication of ZA200800314B publication Critical patent/ZA200800314B/xx

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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/24—Esteramides
    • 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
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero 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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
    • 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
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings
    • C07F9/65392—Five-membered rings containing two nitrogen atoms
    • C07F9/65397—Five-membered rings containing two nitrogen atoms having the two nitrogen atoms in positions 1 and 3
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
ZA200800314A 2005-06-29 2006-06-29 Phosphoramidate alkylator prodrugs ZA200800314B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US69575505P 2005-06-29 2005-06-29

Publications (1)

Publication Number Publication Date
ZA200800314B true ZA200800314B (en) 2009-09-30

Family

ID=37596083

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200800314A ZA200800314B (en) 2005-06-29 2006-06-29 Phosphoramidate alkylator prodrugs

Country Status (24)

Country Link
US (4) US8003625B2 (xx)
EP (2) EP2336141B1 (xx)
JP (2) JP5180824B2 (xx)
KR (1) KR101198571B1 (xx)
CN (2) CN102746336B (xx)
AU (2) AU2006263433B8 (xx)
BR (1) BRPI0612845A8 (xx)
CA (1) CA2613312C (xx)
CY (1) CY1113250T1 (xx)
DK (1) DK1896040T3 (xx)
ES (2) ES2579235T3 (xx)
HK (1) HK1113754A1 (xx)
HR (1) HRP20120803T1 (xx)
IL (1) IL188236A (xx)
NO (1) NO334420B1 (xx)
NZ (1) NZ565378A (xx)
PL (1) PL1896040T3 (xx)
PT (1) PT1896040E (xx)
RS (1) RS52505B (xx)
RU (1) RU2414475C2 (xx)
SI (1) SI1896040T1 (xx)
TW (1) TWI384989B (xx)
WO (1) WO2007002931A2 (xx)
ZA (1) ZA200800314B (xx)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006263433B8 (en) * 2005-06-29 2011-06-09 Immunogenesis, Inc. Phosphoramidate alkylator prodrugs
ES2884044T3 (es) * 2006-12-26 2021-12-10 Immunogenesis Inc Profármaco alquilante de fosforamidato para el tratamiento del cáncer
WO2008124691A1 (en) 2007-04-05 2008-10-16 Threshold Pharmaceuticals, Inc. Glufosfamide combination therapy
WO2009018163A1 (en) * 2007-07-27 2009-02-05 Threshold Pharmaceuticals, Inc. Hypoxia activated prodrugs of anthracyclines
UA104579C2 (uk) * 2007-12-10 2014-02-25 Байокрист Фармасьютикалз, Инк. Спосіб лікування раку кровотворної системи із застосуванням фородезину у комбінації з ритуксимабом
WO2010044885A2 (en) 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
ES2884674T3 (es) 2008-10-21 2021-12-10 Immunogenesis Inc Tratamiento del cáncer con el profármaco activado por hipoxia TH-302 en combinación con docetaxel o pemetrexed
RU2013102398A (ru) * 2010-06-28 2014-08-10 Тресхолд Фармасьютикалз, Инк. Лечение рака крови
ES2649340T3 (es) * 2010-07-12 2018-01-11 Threshold Pharmaceuticals, Inc. Administración de fármacos activados por hipoxia y agentes antiangiogénicos para el tratamiento del cáncer
US20140171389A1 (en) * 2011-04-01 2014-06-19 Threshold Pharmaceuticals, Inc. Methods for treating cancer
AU2012242514A1 (en) * 2011-04-15 2013-10-24 Threshold Pharmaceuticals, Inc. Unit dose form for oral administration
WO2012145684A1 (en) * 2011-04-22 2012-10-26 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Transient hypoxia inducers and their use
CN102850397B (zh) * 2011-06-29 2015-02-18 北京大学 多靶点抗肿瘤化合物及其制备方法和应用
CN102924507A (zh) * 2011-11-10 2013-02-13 安徽四维药业有限公司 一种抗肿瘤化合物及其制备方法与应用、药物组合物
WO2013096687A1 (en) 2011-12-22 2013-06-27 Threshold Pharmaceuticals, Inc. Administration of hypoxia activated prodrugs in combination with chk1 inhibitors for treating cancer
WO2013096684A1 (en) * 2011-12-22 2013-06-27 Threshold Pharmaceuticals, Inc. Hypoxia activated prodrugs and mtor inhibitors for treating cancer
WO2013126539A1 (en) * 2012-02-21 2013-08-29 Threshold Pharmaceuticals Inc. Treatment of cancer
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
KR20150027155A (ko) * 2012-07-03 2015-03-11 브리스톨-마이어스 스큅 컴퍼니 바이러스 감염의 치료를 위한 뉴클레오시드 화합물의 부분입체이성질체적으로 풍부한 포스포르아미데이트 유도체의 제조 방법
WO2014062856A1 (en) 2012-10-16 2014-04-24 Halozyme, Inc. Hypoxia and hyaluronan and markers thereof for diagnosis and monitoring of diseases and conditions and related methods
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US10037382B2 (en) 2012-10-29 2018-07-31 Kyocera Corporation Surface acoustic wave sensor
WO2015013448A1 (en) 2013-07-26 2015-01-29 Threshold Pharmaceuticals, Inc. Treatment of pancreatic cancer with a combination of a hypoxia-acti vated prodrug and a taxane
WO2015025283A2 (en) 2013-08-20 2015-02-26 Stichting Maastricht Radiation Oncology "Maastro-Clinic" Dual action carbonic anhydrase inhibitors
US20160251387A1 (en) 2013-10-10 2016-09-01 Merck Patent Gmbh Synthesis of 1-alkyl-2-amino-imidazol-5-carboxylic acid ester via calpha-substituted n-alkyl-glycine ester derivatives
US10071109B2 (en) 2013-11-06 2018-09-11 Molecular Templates, Inc. Predictive biomarker for hypoxia-activated prodrug therapy
CN104628772A (zh) * 2013-11-07 2015-05-20 四川恒康发展有限责任公司 一种抗肿瘤前药及其激活剂、组合物和应用
CN114404427A (zh) * 2014-02-13 2022-04-29 配体药物公司 前药化合物及其用途
WO2016011195A1 (en) * 2014-07-17 2016-01-21 Threshold Pharmaceuticals, Inc. Th-302 solid forms and methods related thereto
KR102034618B1 (ko) * 2015-03-10 2019-10-21 아센타위츠 파마슈티컬즈 리미티드 Dna 알킬화제
CA2981494C (en) 2015-04-02 2023-09-05 Obi Pharma, Inc. Nitrobenzyl derivatives of anti-cancer agents
PL412787A1 (pl) 2015-06-22 2017-01-02 Magdalena Król Oparty na makrofagach celowany system dostarczania związków związanych z ferrytyną
CN105037427B (zh) * 2015-06-22 2017-05-31 石家庄学院 丹参酮iia亚乙基亚胺磷酸酯衍生物及其制备方法与应用
WO2016210175A1 (en) * 2015-06-24 2016-12-29 Threshold Pharmaceuticals, Inc. Aziridine containing dna alkylating agents
AU2016357728B2 (en) * 2015-11-16 2020-08-27 Obi Pharma, Inc. (R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N'-bis (ethylene)phosphoramidate, compositions and methods for their use and preparation
EP3442979A4 (en) * 2016-04-04 2019-12-18 Rutgers, the State University of New Jersey topoisomerase poisons
LT3565806T (lt) 2017-01-06 2022-06-10 Rivus Pharmaceuticals, Inc. Nauji fenilo dariniai
EP3737676B1 (en) 2018-01-09 2024-03-06 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
US20210283139A1 (en) 2018-06-13 2021-09-16 Amphista Therapeutics Ltd Bifunctional molecules for targeting uchl5
CA3103185A1 (en) 2018-06-13 2019-12-19 Amphista Therapeutics Ltd Bifunctional molecules for targeting rpn11
WO2019238886A1 (en) 2018-06-13 2019-12-19 University Of Dundee Bifunctional molecules for targeting usp14
CN110746459A (zh) * 2018-07-24 2020-02-04 上海喀露蓝科技有限公司 一种艾伏磷酰胺的制备方法
EP3650046A1 (en) 2018-11-08 2020-05-13 Cellis AG Mesenchymal stem cell based targeted active ingredient delivery system
CN109705187B (zh) * 2019-01-29 2021-08-20 石家庄学院 一种雷公藤红素衍生物及其制备方法与应用
CN112755001B (zh) * 2019-11-01 2022-04-12 深圳艾欣达伟医药科技有限公司 口服给药的固体剂型药物
WO2022195092A1 (en) 2021-03-18 2022-09-22 Cellis Ag Ferritin variants with increased stability and complexation ability
JP2023518932A (ja) 2020-03-18 2023-05-09 セリス アーゲー 安定性、複合体形成能力及びトランスフェリン受容体親和性が向上したフェリチン変異体
WO2023025312A1 (zh) 2021-08-27 2023-03-02 深圳艾欣达伟医药科技有限公司 使用th-302治疗parp抑制剂耐药的患者
CN117651548A (zh) 2021-08-27 2024-03-05 深圳艾欣达伟医药科技有限公司 冻干制剂溶液及冻干制剂、方法和用途
WO2024056413A1 (en) 2022-09-13 2024-03-21 Cellis Ag Isolated targeted delivery system for the treatment of glioma

Family Cites Families (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3652579A (en) 1969-06-26 1972-03-28 Hoffmann La Roche 1-methyl-2-substituted 5-nitroimidazoles
DE2229248C3 (de) 1971-07-30 1980-03-27 Gruppo Lepetit S.P.A., Mailand (Italien) 5-Iminomethyl-2-nitroimidazoI-Derivate und Verfahren zu deren Herstellung
US4921963A (en) 1987-04-13 1990-05-01 British Columbia Cancer Foundation Platinum complexes with one radiosensitizing ligand
JPH0819111B2 (ja) 1987-10-22 1996-02-28 ポーラ化成工業株式会社 ２―ニトロイミダゾール誘導体及びこれを有効成分とする放射線増感剤
US5403932A (en) 1988-05-25 1995-04-04 Research Corporation Technologies, Inc. Phosphoramidates useful as antitumor agents
US5190929A (en) 1988-05-25 1993-03-02 Research Corporation Technologies, Inc. Cyclophosphamide analogs useful as anti-tumor agents
US4908356A (en) 1988-05-25 1990-03-13 Research Corporation Technologies, Inc. Aldophosphamide derivatives useful as antitumor agents
DE3835772A1 (de) * 1988-10-20 1990-04-26 Deutsches Krebsforsch Tumorhemmende saccharid-konjugate
JP2626727B2 (ja) 1990-01-26 1997-07-02 ポーラ化成工業株式会社 ２―ニトロイミダゾール誘導体、その製造法及びこれを有効成分とする放射線増感剤
HU9201539D0 (en) 1990-09-11 1992-08-28 Kortec Ag Method and device for gasifying gasifiable materials and/or transforming gas as well as heat exchanger of high temperature for executing said method
US5233031A (en) 1991-09-23 1993-08-03 University Of Rochester Phosphoramidate analogs of 2'-deoxyuridine
JP4115514B2 (ja) 1991-10-23 2008-07-09 キャンサー・リサーチ・キヤンペーン・テクノロジー・リミテツド Ｃｂ １９５４およびその類似体を細胞障害性の形態に還元するための細菌のニトロリダクターゼ
US5750782A (en) 1992-11-27 1998-05-12 Cancer Research Campaign Technology Limited Nitroaniline derivatives and their use as anti-tumour agents
US5306727A (en) * 1993-04-30 1994-04-26 Research Corporation Technologies, Inc. Phosphoramidates useful as antitumor agents
US5691371A (en) 1993-05-25 1997-11-25 Auckland Uniservices Limited Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents
EP0648503B1 (en) 1993-09-22 2000-07-26 Hoechst Aktiengesellschaft Pro-prodrugs, their production and use
JPH07309761A (ja) 1994-05-20 1995-11-28 Kyowa Hakko Kogyo Co Ltd デュオカルマイシン誘導体の安定化法
US5659061A (en) * 1995-04-20 1997-08-19 Drug Innovation & Design, Inc. Tumor protease activated prodrugs of phosphoramide mustard analogs with toxification and detoxification functionalities
GB9516943D0 (en) 1995-08-18 1995-10-18 Cancer Soc Auckland Div Nz Inc Novel cyclopropylindoles and their secoprecursors,and their use as prodrugs
US6218519B1 (en) 1996-04-12 2001-04-17 Pro-Neuron, Inc. Compounds and methods for the selective treatment of cancer and bacterial infections
US5728271A (en) 1996-05-20 1998-03-17 Rti Resource Transforms International Ltd. Energy efficient liquefaction of biomaterials by thermolysis
AU725988C (en) 1996-05-20 2007-11-15 Dynamotive Energy Systems Corporation Energy efficient liquefaction of biomaterials by thermolysis
US6130237A (en) 1996-09-12 2000-10-10 Cancer Research Campaign Technology Limited Condensed N-aclyindoles as antitumor agents
US6251933B1 (en) 1996-12-13 2001-06-26 The Cancer Research Campaign Technology Limited Seco precursors of cyclopropylindolines and their use as prodrugs
DE19720312A1 (de) 1997-05-15 1998-11-19 Hoechst Ag Zubereitung mit erhöhter in vivo Verträglichkeit
US6017948A (en) 1998-10-30 2000-01-25 Supergen, Inc. Water-miscible pharmaceutical compositions
US7914994B2 (en) 1998-12-24 2011-03-29 Cepheid Method for separating an analyte from a sample
US6240925B1 (en) 1999-03-23 2001-06-05 Cynosure, Inc. Photothermal vascular targeting with bioreductive agents
GB9909612D0 (en) 1999-04-26 1999-06-23 Cancer Res Campaign Tech N-protected amines and their use as prodrugs
EP1185276B1 (en) * 1999-05-24 2003-12-10 Southern Research Institute Isophosphoramide mustard analogs and use thereof
CA2377232A1 (en) 1999-06-11 2000-12-21 Henceforth Hibernia, Inc. Prophylactic, therapeutic and industrial antioxidant compositions enhanced with stabilized atomic hydrogen/free electrons and methods to prepare and use such compositions
AU5935600A (en) * 1999-07-14 2001-01-30 Richard F. Borch Phosphoramide compounds
JP2004538240A (ja) 2000-03-31 2004-12-24 パーデュー・リサーチ・ファウンデーション ホスホラミデートおよびそのための方法
EP1243276A1 (en) 2001-03-23 2002-09-25 Franciscus Marinus Hendrikus De Groot Elongated and multiple spacers containing activatible prodrugs
US20030091574A1 (en) 2001-03-23 2003-05-15 Gevas Philip C. Combination treatment of pancreatic cancer
US6506739B1 (en) 2001-05-01 2003-01-14 Telik, Inc. Bis-(N,N'-bis-(2-haloethyl)amino)phosphoramidates as antitumor agents
CN101671335A (zh) 2001-05-31 2010-03-17 梅达莱克斯公司 细胞毒素、其有用的前体药物、连接基团和稳定剂
FR2825926A1 (fr) 2001-06-14 2002-12-20 Sod Conseils Rech Applic Derives d'imidazoles modulant les canaux sodiques
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
KR20030067275A (ko) 2002-02-07 2003-08-14 주식회사 하이폭시 니트로이미다졸 및 위상 이성질화 효소 저해제를유효성분으로 포함하는 항암제
US20040009667A1 (en) 2002-02-07 2004-01-15 Etsuo Iijima Etching method
EP1487972B1 (en) 2002-02-21 2015-08-12 Institute Of Virology Mn/ca ix-specific monoclonal antibodies generated from mn/ca ix-deficient mice and methods of use
JP4227771B2 (ja) 2002-07-17 2009-02-18 三菱重工業株式会社 バイオマスのガス化方法
US6833390B2 (en) 2002-07-22 2004-12-21 Bayer Polymers Llc Process for preparing closed-cell water-blown rigid polyurethane foams having improved mechanical properties
DE10237931A1 (de) 2002-08-14 2004-02-26 Endress + Hauser Gmbh + Co. Kg Vorrichtung zur Überwachung eines vorbestimmten Füllstands eines Messmediums in einem Behälter
AU2004203977B2 (en) 2003-01-09 2010-06-17 Pfizer Inc. Diazepinoindole derivatives as kinase inhibitors
GB0306907D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Boireductively-activated prodrugs
GB0306908D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Bioreductively activated stilbene prodrugs
ZA200507752B (en) 2003-03-28 2007-01-31 Threshold Pharmaceuticals Inc Compositions and methods for treating cancer
US6855695B2 (en) 2003-06-13 2005-02-15 Vion Pharmaceuticals, Inc. Water-soluble SHPs as novel alkylating agents
US7340059B2 (en) 2003-06-17 2008-03-04 Intel Corporation Programmable scrambler and De-scrambler for digital telephony equipment
JP2005041733A (ja) 2003-07-28 2005-02-17 National Institute Of Advanced Industrial & Technology バイオマスによる水素製造法
CN1917885A (zh) 2004-02-06 2007-02-21 施瑞修德制药公司 抗癌疗法
US7432106B2 (en) 2004-03-24 2008-10-07 Applied Biosystems Inc. Liquid processing device including gas trap, and system and method
AU2005241093B2 (en) 2004-05-04 2008-06-05 Institute Of Virology Of Slovak Academy Of Sciences MN/CA IX/ CA9 and renal cancer prognosis
IL162713A (en) 2004-06-24 2011-04-28 Desalitech Ltd Apparatus and methods for continuous desalination in closed circuit without containers
TW200612918A (en) 2004-07-29 2006-05-01 Threshold Pharmaceuticals Inc Lonidamine analogs
TW200605885A (en) 2004-07-29 2006-02-16 Threshold Pharmaceuticals Inc Multicyclic lonidamine analogs
MX2007006102A (es) 2004-11-22 2007-07-11 Threshold Pharmaceuticals Inc Agentes anti-cancer de union a tubulina y profarmacos de los mismos.
US20070117784A1 (en) 2005-03-04 2007-05-24 Novacea, Inc. Treatment of hyperproliferative diseases with anthraquinones
AU2006263433B8 (en) 2005-06-29 2011-06-09 Immunogenesis, Inc. Phosphoramidate alkylator prodrugs
EP1931769A2 (en) 2005-10-03 2008-06-18 Genetix Pharmaceuticals Inc. Method for selectively depleting hypoxic cells
WO2008011588A2 (en) 2006-07-20 2008-01-24 Threshold Pharmaceuticals, Inc. Glycoconjugates of phosphoramidate alkylators for treatment of cancer
WO2008033041A1 (en) 2006-09-11 2008-03-20 Auckland Uniservices Limited Cancer treatment
JP2008069017A (ja) 2006-09-12 2008-03-27 Matsushita Electric Ind Co Ltd 水素製造方法
US7807454B2 (en) 2006-10-18 2010-10-05 The Regents Of The University Of California Microfluidic magnetophoretic device and methods for using the same
WO2008076826A1 (en) 2006-12-13 2008-06-26 Threshold Pharmaceuticals, Inc. Pyrophosphoramide alkylators
ES2884044T3 (es) 2006-12-26 2021-12-10 Immunogenesis Inc Profármaco alquilante de fosforamidato para el tratamiento del cáncer
JP5174411B2 (ja) 2007-09-28 2013-04-03 独立行政法人石油天然ガス・金属鉱物資源機構 管式リフォーマーの有効熱利用方法
US8216607B2 (en) 2008-03-17 2012-07-10 Roger Williams Hospital Combination of ceramide and gemcitabine for inducing cell death and uses thereof in treating cancer
JP5731372B2 (ja) 2008-04-10 2015-06-10 ヴァージニア コモンウェルス ユニバーシティ 癌治療用腫瘍低酸素の誘発
US8501765B2 (en) 2008-06-11 2013-08-06 Genentech, Inc. Diazacarbazoles and methods of use
JP4665021B2 (ja) 2008-09-03 2011-04-06 三菱重工業株式会社 バイオマスのガス化方法
ES2884674T3 (es) 2008-10-21 2021-12-10 Immunogenesis Inc Tratamiento del cáncer con el profármaco activado por hipoxia TH-302 en combinación con docetaxel o pemetrexed
EP2409130B1 (en) 2009-03-20 2013-12-04 Pbs Biotech, Inc. Automatable aseptic sample withdrawal system
US20120114637A1 (en) 2009-05-04 2012-05-10 Santen Pharmaceutical Co., Ltd. Mtor pathway inhibitors for treating ocular disorders
AU2010314905A1 (en) 2009-11-06 2012-05-24 Infinity Pharmaceuticals, Inc. Oral formulations of a hedgehog pathway inhibitor
JP5659536B2 (ja) 2010-03-31 2015-01-28 新日鐵住金株式会社 タール含有ガスの改質用触媒及びその製造方法、並びにタール含有ガスの改質方法
RU2013102398A (ru) 2010-06-28 2014-08-10 Тресхолд Фармасьютикалз, Инк. Лечение рака крови
ES2649340T3 (es) 2010-07-12 2018-01-11 Threshold Pharmaceuticals, Inc. Administración de fármacos activados por hipoxia y agentes antiangiogénicos para el tratamiento del cáncer
US10357577B2 (en) 2010-07-16 2019-07-23 Auckland Uniservices Limited Bacterial nitroreductase enzymes and methods relating thereto
US20140171389A1 (en) 2011-04-01 2014-06-19 Threshold Pharmaceuticals, Inc. Methods for treating cancer
AU2012242514A1 (en) 2011-04-15 2013-10-24 Threshold Pharmaceuticals, Inc. Unit dose form for oral administration
JP5805989B2 (ja) 2011-04-26 2015-11-10 大塚電子株式会社 電気泳動移動度測定用セル並びにそれを用いた測定装置及び測定方法
WO2013094382A1 (ja) 2011-12-20 2013-06-27 学校法人長崎総合科学大学 合成ガスの生成方法及び製造装置、並びに、液体燃料の合成方法及び合成装置
WO2013096684A1 (en) 2011-12-22 2013-06-27 Threshold Pharmaceuticals, Inc. Hypoxia activated prodrugs and mtor inhibitors for treating cancer
JP2015511226A (ja) 2012-01-31 2015-04-16 スレッショルド ファーマシューティカルズ，インコーポレイテッド 低酸素活性化プロドラッグ療法のための予測バイオマーカー

Also Published As

Publication number Publication date
KR101198571B1 (ko) 2012-11-07
SI1896040T1 (sl) 2012-12-31
US9226932B2 (en) 2016-01-05
US8664204B2 (en) 2014-03-04
KR20080027901A (ko) 2008-03-28
WO2007002931A3 (en) 2009-04-23
CN101501054A (zh) 2009-08-05
CN102746336B (zh) 2015-08-19
TW200800228A (en) 2008-01-01
TWI384989B (zh) 2013-02-11
US20100137254A1 (en) 2010-06-03
BRPI0612845A2 (pt) 2010-11-30
AU2006263433A1 (en) 2007-01-04
EP1896040B1 (en) 2012-08-01
ES2579235T3 (es) 2016-08-08
IL188236A0 (en) 2008-08-07
CN101501054B (zh) 2012-09-05
US8003625B2 (en) 2011-08-23
EP1896040A2 (en) 2008-03-12
JP2012153722A (ja) 2012-08-16
AU2006263433B8 (en) 2011-06-09
AU2011202075B2 (en) 2013-01-17
US20140170240A1 (en) 2014-06-19
NO20080442L (no) 2008-03-31
HK1113754A1 (en) 2008-10-17
EP2336141A2 (en) 2011-06-22
NZ565378A (en) 2011-03-31
JP5781007B2 (ja) 2015-09-16
IL188236A (en) 2011-11-30
AU2011202075A1 (en) 2011-05-26
JP5180824B2 (ja) 2013-04-10
CN102746336A (zh) 2012-10-24
NO334420B1 (no) 2014-03-03
RU2008103195A (ru) 2009-08-10
PT1896040E (pt) 2012-09-27
RS52505B (en) 2013-04-30
BRPI0612845A8 (pt) 2018-01-23
EP2336141A3 (en) 2011-09-14
US20130303778A1 (en) 2013-11-14
HRP20120803T1 (hr) 2012-11-30
ES2389532T3 (es) 2012-10-29
EP1896040A4 (en) 2010-02-10
US8507464B2 (en) 2013-08-13
CA2613312A1 (en) 2007-01-04
WO2007002931A2 (en) 2007-01-04
JP2009502743A (ja) 2009-01-29
CY1113250T1 (el) 2016-04-13
DK1896040T3 (da) 2012-09-03
US20110251159A1 (en) 2011-10-13
CA2613312C (en) 2014-10-14
RU2414475C2 (ru) 2011-03-20
AU2006263433B2 (en) 2011-06-02
AU2011202075A8 (en) 2013-05-30
EP2336141B1 (en) 2016-03-30
PL1896040T3 (pl) 2012-12-31
AU2011202075B8 (en) 2013-05-30

Similar Documents

Publication Publication Date Title
ZA200800314B (en) Phosphoramidate alkylator prodrugs
SI1968612T1 (sl) Dinukleotid predzdravila
GB0306907D0 (en) Boireductively-activated prodrugs
ZA200810400B (en) Antiviral phosphinate compounds
EP1955129A4 (en) MULTIPLE CONTROL SCREENS
ZA201004371B (en) Efficient aspirin prodrugs
GB2428232B (en) Traction arrangements
HK1135989A1 (en) Polyfluoroether-based phosphates
EP2118052A4 (en) NEW PRODRUGS
AP2008004705A0 (en) Pnem prodrugs
GB0421294D0 (en) Bioreductively-activated prodrugs
GB0515699D0 (en) Prodrugs
ZA200805660B (en) Heteroaromatic sulfonamide prodrugs
GB0421296D0 (en) Bioreductively-activated prodrugs
GB0503952D0 (en) A cable arrangement
HK1113065A1 (en) Sole member
GB0414567D0 (en) Prodrugs
GB0421295D0 (en) Bioreductively-activated prodrugs
GB0526010D0 (en) Phosphorus compounds
ZA201107393B (en) Antiviral phosphinate compounds
AP2008004721A0 (en) Antiviral phosphinate compounds
GB0622798D0 (en) Phosphorus compounds
GB0508366D0 (en) Cables
GB0702469D0 (en) Just one more 28
GB0702067D0 (en) Just one more 5