DK2750768T3 - Decitabinderivatformuleringer - Google Patents

Decitabinderivatformuleringer Download PDF

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Publication number
DK2750768T3
DK2750768T3 DK12759857.1T DK12759857T DK2750768T3 DK 2750768 T3 DK2750768 T3 DK 2750768T3 DK 12759857 T DK12759857 T DK 12759857T DK 2750768 T3 DK2750768 T3 DK 2750768T3
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compound
salt
formulation
dmso
acid
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DK12759857.1T
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English (en)
Inventor
Rajashree Joshi-Hangal
Chunlin Tang
Sanjeev Redkar
Harish Ravivarapu
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Astex Pharmaceuticals Inc
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    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K31/7084—Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
    • 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
    • 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
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • 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
    • 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
    • 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
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic acid
    • A61K31/708—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 containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)

Claims (20)

1. Formulering, der omfatter: (a) en forbindelse med formlen:
eller et farmaceutisk acceptabelt salt deraf; opløst i (b) et i det væsentlige vandfrit opløsningsmiddel, der omfatter 60 % til 70 % propylenglycol; 20 % til 30 % glycerin og 5 % til 15 % ethanol (w/w/w).
2. Formulering ifølge 1, hvor opløsningsmidlet er 65 % propylenglycol; 25 % glycerin og 10 % ethanol (w/w/w).
3. Formulering ifølge et hvilket som helst af de foregående krav, hvor saltet er et natriumsalt.
4. Formulering ifølge et hvilket som helst af de foregående krav, hvor forbindelsen er til stede i en koncentration på fra 80 mg/ml til 110 mg/ml, eventuelt på omkring 100 mg/ml.
5. Formulering ifølge et hvilket som helst af de foregående krav, som yderligere omfatter DMSO, eventuelt i et DMSO:forbindelse-forhold på omkring 2:omkring 1; omkring 1:omkring 1; omkring 0,5:omkring 1; omkring 0,3:omkring 1 eller 0,2 - 0,3:omkring 1.
6. Formulering ifølge et hvilket som helst af de foregående krav, som er egnet til indgivelse ved subkutan injektion.
Ί. Kit, der omfatter: (a) en første beholder, der indeholder en forbindelse som defineret i krav 1 eller krav 3; og (b) en anden beholder, der indeholder et i det væsentlige vandfrit opløsningsmiddel som defineret i krav 1 eller 2.
8. Kit ifølge krav 7, hvor forbindelsen er lyofiliseret.
9. Kit ifølge et hvilket som helst af kravene 7-8, hvor den første beholder indeholder 80 mg til 110 mg af forbindelsen.
10. Kit ifølge et hvilket som helst af kravene 7-9, hvor den første beholder indeholder omkring 100 mg af forbindelsen.
11. Kit ifølge et hvilket som helst af kravene 7-10, der yderligere omfatter instruktioner i indgivelse ved subkutan injektion.
12. Kit ifølge et hvilket som helst af kravene 7-11, hvor forbindelsen er i form af et i det væsentlige vandfrit pulver.
13. Kit ifølge krav 12, hvor det i det væsentlige vandfrie pulver hovedsagelig består af forbindelsen og DMSO, idet DMSO er til stede i en mængde på op til 200 % w/w.
14. Kit ifølge krav 13, hvor DMSO er til stede i en mængde på 20-30% w/w DMSO/forbindelse.
15. Fremgangsmåde til fremstilling af en farmaceutisk sammensætning, hvilken fremgangsmåde omfatter at opløse en forbindelse som defineret i krav 1 eller krav 3 i et i det væsentlige vandfrit opløsningsmiddel som defineret i krav 1 eller 2.
16. Fremgangsmåde ifølge krav 15, der yderligere omfatter trinnene: (a) at opløse forbindelsen i DMSO for at opnå en opløsning af forbindelsen i DMSO; og (b) at lyofilisere opløsningen fra trin (a) for at tilvejebringe forbindelsen som et i det væsentlige vandfrit pulver.
17. Formulering ifølge et hvilket som helst af kravene 1-6 eller kit ifølge et hvilket som helst af kravene 7-14 til anvendelse ved behandling af cancer, myelodysplastisk syndrom, leukæmi eller en solid tumor.
18. Formulering ifølge et hvilket som helst af kravene 1-6 eller kit ifølge et hvilket som helst af kravene 7-14 til anvendelse ved behandling af brystcancer, hudcancer, knoglecancer, prostatacancer, levercancer, lungecancer, hjernecancer, cancer af strubehovedet, galdeblæren, pankreas, rectum, parathyreoidea, thyreoidea, binyren, nervevæv, hoved og hals, colon, mave, bronkier, nyrer, basalcellekarcinom, pladecellekarcinom af både den ulcererende og den papilære type, metastatisk hudkarcinom, osteosarkom, Ewings sarkom, veticulumcellesarkom, myelom, kæmpeceiletumor, småcellet lungetumor, galdesten, ø-celletumor, primær hjernetumor, akutte og kroniske lymfatiske og granulocytiske tumorer, hårcelletumor, adenom, hyperplasi, medullært karcinom, fæokromocytom, slimhindeneuromer, intestinale ganglioneuromer, hyperplastisk hornhindenervetumor, marfanoid habitus-tumor, Wilms tumor, seminom, ovarietumor, leiomyomater-tumor, cervikal dysplasi og in situ-karcinom, neuroblastom, retinoblastom, blødvævssarkom, malignt carcinoid, topisk hudlæsion, mycosis fungoides, rhabdomyosarkom, Kaposis sarkom, osteogene og andre sarkomer, malign hyperkalcæmi, renalcelletumor, polycythermia vera, adenocarkarcinom, glioblastoma multiforme, leukæmier, lymfomer, maligne melanomer, epidermoide karcinomer eller andre karcinomer og sarkomer.
19. Formulering eller kit til anvendelse ifølge krav 17, hvor leukæmien er valgt blandt akut myeloid leukæmi (AML), akut promyelocytisk leukæmi (APML), akut lymfoblastisk leukæmi (ALL) og kronisk myelogen leukæmi (CML).
20. Formulering ifølge et hvilket som helst af kravene 1-6, eller kit ifølge et hvilket som helst af kravene 7-14, til anvendelse ved behandling af en lidelse forbundet med unormal hæmoglobinsyntese.
21. Formulering eller kit til anvendelse ifølge et hvilket som helst af kravene 17 til 19, hvor formuleringen er til subkutan indgivelse.
DK12759857.1T 2011-08-30 2012-08-29 Decitabinderivatformuleringer DK2750768T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161529081P 2011-08-30 2011-08-30
PCT/US2012/052816 WO2013033176A1 (en) 2011-08-30 2012-08-29 Decitabine derivative formulations

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DK2750768T3 true DK2750768T3 (da) 2019-01-21

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US (4) US9381207B2 (da)
EP (2) EP3431142B1 (da)
JP (2) JP6038921B2 (da)
KR (1) KR102004559B1 (da)
CN (2) CN103945902B (da)
AU (2) AU2012302051B2 (da)
BR (1) BR112014004779B1 (da)
CA (1) CA2845585C (da)
CO (1) CO6950470A2 (da)
CY (1) CY1122168T1 (da)
DK (1) DK2750768T3 (da)
ES (1) ES2702495T3 (da)
HK (1) HK1199715A1 (da)
HU (1) HUE042327T2 (da)
IL (2) IL231209A0 (da)
LT (1) LT2750768T (da)
MX (1) MX359314B (da)
MY (2) MY163296A (da)
PH (1) PH12018501678A1 (da)
PL (1) PL2750768T3 (da)
PT (1) PT2750768T (da)
RU (1) RU2605289C2 (da)
SG (1) SG2014013395A (da)
UA (1) UA116528C2 (da)
WO (1) WO2013033176A1 (da)
ZA (1) ZA201701083B (da)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7700567B2 (en) 2005-09-29 2010-04-20 Supergen, Inc. Oligonucleotide analogues incorporating 5-aza-cytosine therein
US10166142B2 (en) 2010-01-29 2019-01-01 Forsight Vision4, Inc. Small molecule delivery with implantable therapeutic device
CA2818612C (en) 2010-11-19 2020-12-29 Forsight Vision4, Inc. Therapeutic agent formulations for implanted devices
WO2013033176A1 (en) * 2011-08-30 2013-03-07 Astex Pharmaceuticals, Inc. Decitabine derivative formulations
KR20150125963A (ko) * 2013-03-01 2015-11-10 아스텍스 파마수티컬스, 인크. 약물 조합체
AU2014236455B2 (en) 2013-03-14 2018-07-12 Forsight Vision4, Inc. Systems for sustained intraocular delivery of low solubility compounds from a port delivery system implant
JP2017524034A (ja) 2014-08-08 2017-08-24 フォーサイト・ビジョン フォー・インコーポレーテッドＦｏｒｓｉｇｈｔ Ｖｉｓｉｏｎ４， Ｉｎｃ． 受容体型チロシンキナーゼ阻害剤の安定で可溶な製剤およびその調製の方法
BR112018000054A2 (pt) * 2015-07-02 2018-09-04 Otsuka Pharmaceutical Co., Ltd. composições farmacêuticas liofilizadas
GB201704966D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201704965D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
KR20200035438A (ko) 2017-08-03 2020-04-03 오쓰까 세이야꾸 가부시키가이샤 약물 화합물 및 이의 정제 방법
CA3211506A1 (en) 2018-02-07 2019-08-15 Lovelace Biomedical Research Institute Inhalable dry powder cytidine analogue composition and method of use as a treatment for cancer
EP3801465B1 (en) 2018-06-11 2024-07-24 The Regents of the University of California Viral vector encoding elovl2 protein for treating age-related macular degeneration
KR20220083704A (ko) * 2019-10-18 2022-06-20 후지필름 와코 준야쿠 가부시키가이샤 포스포아미다이트 활성화제
WO2022002905A1 (en) * 2020-07-01 2022-01-06 Sandoz Ag Parenteral pharmaceutical composition comprising azacitidine in dmso

Family Cites Families (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133858A (en) * 1954-03-24 1964-05-19 Abbott Lab Stable thiobarbituric acid solution
CH527207A (de) 1968-05-08 1972-08-31 Ceskoslovenska Akademie Ved Verfahren zur Herstellung von 1-Glycosyl-5-azacytosinen
DE2105468A1 (en) 1970-04-23 1971-11-18 Czeskoslovenska akademie ved, Prag; VtnKarstedt, E., Dipl.-Ing. Dr., Pat-Anw., 4200 Oberhausen 1-glycosyl-5-aza-cytosines prepn
US5157120A (en) 1980-09-16 1992-10-20 Syntex (U.S.A.) Inc. Guanine derivatives
US4855304A (en) 1985-01-10 1989-08-08 Repligen Corporation Dinucleoside pyrophosphates and pyrophosphate homologs as plant antivirals
JPS61176523A (ja) 1985-01-30 1986-08-08 Teruhiko Beppu 制癌剤
GB8612826D0 (en) 1986-05-27 1986-07-02 Boots Co Plc Insecticidal compositions
DE3712786A1 (de) 1987-04-15 1988-11-03 Merck Patent Gmbh Verfahren und mittel zur bestimmung von nucleinsaeuren
CS269077B1 (cs) 1987-10-01 1990-04-11 Piskala Alois Způsob přípravy 5-azacytosinů
US5736531A (en) 1987-10-28 1998-04-07 Pro-Neuron, Inc. Compositions of chemotherapeutic agent or antiviral agent with acylated pyrimidine nucleosides
US5968914A (en) 1987-10-28 1999-10-19 Pro-Neuron, Inc. Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides
US4904770A (en) 1988-03-24 1990-02-27 Bristol-Myers Company Production of 2',3'-dideoxy-2',3'-didehydronucleosides
US5324831A (en) 1988-04-06 1994-06-28 The United States Of America As Represented By The Secretary Of Health And Human Services Phosphoramidite reagent for chemical synthesis of modified DNA
PT93772A (pt) 1989-04-17 1991-01-08 Searle & Co Processo para a preparacao de composicoes para o tratamento de neoplasias, contendo um agente anti-neoplastico, por exemplo doxorubicina e um agente protector para reduzir os efeitos secundarios, por exemplo carbetimer
ZA923640B (en) 1991-05-21 1993-02-24 Iaf Biochem Int Processes for the diastereoselective synthesis of nucleosides
EP0594667B1 (en) 1991-07-05 2001-09-19 Pro-Neuron, Inc. Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides
IL103311A0 (en) 1991-10-07 1993-03-15 Univ Johns Hopkins Formation of triple helix complexes of single stranded nucleic acids using nucleoside oligomers
JPH05219974A (ja) 1992-02-13 1993-08-31 Mitsui Petrochem Ind Ltd トロパンアルカロイドの製造方法
JPH05246891A (ja) * 1992-03-09 1993-09-24 Kobayashi Seiyaku Kogyo Kk 安定な抗膵炎用注射液
US5607691A (en) 1992-06-12 1997-03-04 Affymax Technologies N.V. Compositions and methods for enhanced drug delivery
WO1994026761A1 (en) 1993-05-14 1994-11-24 Pro-Neuron, Inc. Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides
GB9311252D0 (en) 1993-06-01 1993-07-21 Hafslund Nycomed As Cell growth regualtors
EP1352956A1 (en) 1993-11-30 2003-10-15 McGILL UNIVERSITY Inhibition of DNA methyltransferase
US6432924B1 (en) 1993-12-26 2002-08-13 East Carolina University Method of treating disorders characterized by overexpression of cytidine deaminase or deoxycytidine deaminase
US5856090A (en) 1994-09-09 1999-01-05 The Scripps Research Institute DNA-methylase linking reaction
US20030104576A1 (en) 1994-10-07 2003-06-05 Jonathan W. Nyce Dna construct, composition, formulations & methods for making the construct & for modulating expression
WO1996036693A1 (en) 1995-05-19 1996-11-21 Phytera, Inc. Manipulation of plant cell and tissue cultures
DE69637669D1 (de) 1995-06-06 2008-10-16 Osiris Therapeutics Inc Myogene differenzierung menschlicher mesenchymaler stammzellen
CA2241255A1 (en) 1995-12-22 1997-07-03 East Carolina University Method of treating disorders characterized by overexpression of cytidine deaminase or deoxycytidine deaminase
KR100398923B1 (ko) 1996-10-16 2003-09-19 아이씨엔 파마슈티컬스, 인코포레이티드 모노시클릭 ｌ-누클레오시드, 이의 유사체 및 이들의 용도
US6423692B2 (en) 1997-04-24 2002-07-23 Dana-Farber Cancer Institute, Inc. Method of enhancing the effectiveness of DCK phosphorylated molecules
US6153383A (en) 1997-12-09 2000-11-28 Verdine; Gregory L. Synthetic transcriptional modulators and uses thereof
SI1659179T1 (sl) 1998-02-05 2011-10-28 Glaxosmithkline Biolog Sa S tumorjem povezani antigenski derivati iz MAGE druĹľine in zaporedja nukleinskih kislin, ki jih kodirajo, uporabni za pripravo fuzijskih proteinov in sestavkov za cepljenje
EP1123111B1 (en) 1998-10-19 2004-09-15 Methylgene, Inc. Modulation of dna methyltransferase expression by combination therapy
DK1141028T3 (da) 1998-12-23 2010-05-25 Pfizer Humane monoklonale antistoffer til CTLA-4
WO2000040269A2 (en) 1999-01-05 2000-07-13 Lee Clarence C Pharmaceutical compositions for treatment of diseased tissues
WO2000062075A1 (en) 1999-04-13 2000-10-19 Rutgers, The State University Of New Jersey Ubiquitin cross-reactive protein as a prognostic marker for tumor cell chemosensitivity
IL146872A0 (en) 1999-06-03 2002-08-14 Methods and compositions for modulating cell proliferation and cell death
DE19935303A1 (de) 1999-07-28 2001-02-08 Aventis Pharma Gmbh Oligonukleotide zur Inhibierung der Expression von humanem eg5
ATE354655T1 (de) 1999-08-24 2007-03-15 Medarex Inc Humane antikörper gegen ctla-4 und deren verwendungen
JP2001163776A (ja) * 1999-09-30 2001-06-19 Nisshin Oil Mills Ltd:The 安定化された液剤
CA2386476A1 (en) 1999-10-18 2001-04-26 Emory University Tms1 compositions and methods of use
WO2001069262A1 (en) 2000-03-15 2001-09-20 University Of Massachusetts ERβ-MEDIATED GENE EXPRESSION
WO2002021140A1 (en) 2000-09-08 2002-03-14 Metabolic Engineering Laboratories Co., Ltd. Nucleic acid sequences and proteins involved in cellular senescence
AU2002239282A1 (en) * 2000-11-28 2002-06-11 Transform Pharmaceuticals, Inc. Pharmaceutical formulations comprising paclitaxel, derivatives, and pharmaceutically acceptable salts thereof
US20040092583A1 (en) 2001-01-02 2004-05-13 Elizabeth Shanahan-Prendergast Treatment for inhibiting neoplastic lesions
EP2360166A1 (en) 2001-01-22 2011-08-24 Merck Sharp & Dohme Corp. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
JP2002223753A (ja) 2001-01-30 2002-08-13 Hitachi Ltd 薬物応答解析用オリゴヌクレオチドアレイ
ATE308335T1 (de) 2001-02-05 2005-11-15 Innoventus Project Ab Histidine-rich glycoprotein (hrgp) zur hemmung der angiogenese
US6613753B2 (en) 2001-02-21 2003-09-02 Supergen, Inc. Restore cancer-suppressing functions to neoplastic cells through DNA hypomethylation
WO2002069903A2 (en) 2001-03-06 2002-09-12 Biocryst Pharmaceuticals, Inc. Nucleosides, preparation thereof and use as inhibitors of rna viral polymerases
US20060194275A1 (en) 2001-04-13 2006-08-31 Incyte Corporation Transporter and ion channels
US6905669B2 (en) 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
NZ528994A (en) 2001-04-26 2006-02-24 Control Delivery Sys Inc Sustained release drug delivery system containing codrugs
US20030148973A1 (en) 2001-05-23 2003-08-07 Peter Emtage MAGE-A1 peptides for treating or preventing cancer
EP1402071A4 (en) 2001-06-08 2005-12-14 Us Genomics Inc METHOD AND PRODUCTS FOR THE ANALYSIS OF NUCLEIC ACIDS BASED ON THE METHYLATION STATUS
JP2002370939A (ja) 2001-06-12 2002-12-24 Taisho Pharmaceut Co Ltd 育毛剤
SE518759C2 (sv) 2001-07-27 2002-11-19 Geneinvent Bbl Ab Vektorer motståndskraftiga mot metylering
US20030045497A1 (en) 2001-07-27 2003-03-06 Geneinvent Bbl Ab Methylation resistant vectors
WO2003012085A1 (en) 2001-07-30 2003-02-13 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Antigen presenting cells, method for their preparation and their use for cancer vaccines
ATE451106T1 (de) 2001-09-05 2009-12-15 Chemgenex Pharmaceuticals Ltd Behandlung von sti571-resistenter oder - intoleranter chronischer myelogener leukemie mittels homoharringtonine alein oder in kombination mit anderen substanzen
US20030158598A1 (en) 2001-09-17 2003-08-21 Control Delivery Systems, Inc. System for sustained-release delivery of anti-inflammatory agents from a coated medical device
IN2014DN10834A (da) 2001-09-17 2015-09-04 Psivida Inc
IL161036A0 (en) 2001-09-24 2004-08-31 Methods and compositions to determine the chemosensitizing dose of suramin used in combination therapy
US7432050B2 (en) 2001-10-05 2008-10-07 Case Western Reserve University Methods and compositions for detecting colon cancers
KR100616369B1 (ko) 2001-11-08 2006-08-28 도꾸리쯔교세이호징 가가꾸 기쥬쯔 신꼬 기꼬 벼의 트랜스포존 유전자
BR0214386A (pt) 2001-11-23 2004-11-30 Chugai Pharmaceutical Co Ltd Método para identificação de enzimas de objetivação a tumor
IL161832A0 (en) 2001-11-29 2005-11-20 Dandrit Biotech As Pharmaceutical composition for inducing an immune response in a human or animal
US20050080027A1 (en) 2001-11-30 2005-04-14 Markus Horer Optimized production of viral vectors derived from paroviruses in packaging and production cells by hsv infection or treatment with dna methylation inhibitors
GB0201498D0 (en) 2002-01-23 2002-03-13 Biotech Res Ventures Pte Ltd Materials and methods for treating cancer
US6998391B2 (en) 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
US20030147813A1 (en) 2002-02-07 2003-08-07 John Lyons Method for treating chronic myelogenous leukemia
AU2002238874A1 (en) 2002-03-13 2003-09-22 F.Hoffmann-La Roche Ag Method for selecting drug sensitivity-determining factors and method for predicting drug sensitivity using the selected factors
JP2003310293A (ja) 2002-04-26 2003-11-05 Mitsui Chemicals Inc ヌクレオシド化合物の製造法
SG165158A1 (en) 2002-05-02 2010-10-28 Wyeth Corp Calicheamicin derivative-carrier conjugates
EP1551437A4 (en) 2002-06-05 2006-03-29 Univ Case Western Reserve METHOD AND COMPOSITIONS FOR DETECTING CANCER
US6982253B2 (en) 2002-06-05 2006-01-03 Supergen, Inc. Liquid formulation of decitabine and use of the same
AU2003286836A1 (en) 2002-10-31 2004-06-07 Supergen, Inc. Pharmaceutical formulations targeting specific regions of the gastrointestinal tract
US20050037992A1 (en) 2003-07-22 2005-02-17 John Lyons Composition and method for treating neurological disorders
US20050059682A1 (en) 2003-09-12 2005-03-17 Supergen, Inc., A Delaware Corporation Compositions and methods for treatment of cancer
WO2005033278A2 (en) 2003-09-30 2005-04-14 Ludwig Institute For Cancer Research In vivo efficacy of ny-eso-1 plus iscom
US7846436B2 (en) 2003-11-28 2010-12-07 Chemgenes Corporation Oligonucleotides and related compounds
US20050266012A1 (en) 2004-05-26 2005-12-01 Jean-Marie Andrieu Compositions comprising demethylating agents as enhancers of immunotherapy for the treatment of chronic infections and neoplastic diseases and methods for treating the same
US20060014949A1 (en) 2004-07-13 2006-01-19 Supergen Inc. Compositions and formulations of decitabine polymorphs and methods of use thereof
US20060069060A1 (en) 2004-09-27 2006-03-30 Sanjeev Redkar Salts of decitabine
US20060063735A1 (en) 2004-09-17 2006-03-23 Supergen, Inc. Salts of 5-azacytidine
EP1819735A1 (en) 2004-11-04 2007-08-22 Pfizer Products Inc. Ctla-4 antibody and aromatase inhibitor or combination treatment for breast cancer
US20060128653A1 (en) 2004-12-10 2006-06-15 Chunlin Tang Pharmaceutical formulation of decitabine
US20060128654A1 (en) 2004-12-10 2006-06-15 Chunlin Tang Pharmaceutical formulation of cytidine analogs and derivatives
EP1833506B1 (en) 2004-12-29 2015-08-26 Mannkind Corporation Use of compositions comprising various tumor-associated antigens as anti-cancer vaccines
US7250416B2 (en) 2005-03-11 2007-07-31 Supergen, Inc. Azacytosine analogs and derivatives
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
US8008449B2 (en) 2005-05-09 2011-08-30 Medarex, Inc. Human monoclonal antibodies to programmed death 1 (PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
CA3201163A1 (en) 2005-07-01 2007-01-11 E. R. Squibb & Sons, L.L.C. Human monoclonal antibodies to programmed death ligand 1 (pd-l1)
US7700567B2 (en) 2005-09-29 2010-04-20 Supergen, Inc. Oligonucleotide analogues incorporating 5-aza-cytosine therein
US20070105792A1 (en) 2005-11-04 2007-05-10 Dimartino Jorge F Administration Of DNA Methylation Inhibitors For Treating Epigenetic Diseases
US20070117776A1 (en) 2005-11-04 2007-05-24 John Lyons Low Dose Therapy Of DNA Methylation Inhibitors
CN101637444B (zh) * 2006-03-17 2012-08-15 山东蓝金生物工程有限公司 含吉西他滨的抗癌药物缓释注射剂
US20090142337A1 (en) * 2006-05-08 2009-06-04 Astex Therapeutics Limited Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment
US8003324B2 (en) * 2007-10-18 2011-08-23 U.S. Department Of Veterans Affairs Modulation of sodium channels by nicotinamide adenine dinucleotide
CN101570553B (zh) * 2008-05-04 2012-03-28 上海医药工业研究院 一种2-脱氧-d-核糖的衍生物及其制备方法和用途
CN101361718B (zh) * 2008-09-26 2013-08-28 深圳万乐药业有限公司 稳定的地西他滨冻干制剂的制备方法
CN101787046B (zh) * 2010-02-11 2012-12-26 福建南方制药股份有限公司 地西他滨的中间体化合物的制备方法
GB201006096D0 (en) 2010-04-13 2010-05-26 Alligator Bioscience Ab Novel compositions and uses thereof
JP6121904B2 (ja) 2010-09-08 2017-04-26 ハロザイム インコーポレイテッド 条件的活性治療用タンパク質を評価および同定する、または発展させる方法
CN101966157B (zh) * 2010-10-14 2013-08-14 苏州特瑞药业有限公司 一种地西他滨缓释微球及其制备方法
AU2012241373B2 (en) 2011-04-15 2016-06-09 Compugen Ltd. Polypeptides and polynucleotides, and uses thereof for treatment of immune related disorders and cancer
WO2013033176A1 (en) 2011-08-30 2013-03-07 Astex Pharmaceuticals, Inc. Decitabine derivative formulations
EP2811984B1 (en) 2012-02-06 2015-08-26 Fresenius Kabi Oncology Limited Process for preparing stable pharmaceutical compositions of compounds susceptible to hydrolysis
KR20150125963A (ko) 2013-03-01 2015-11-10 아스텍스 파마수티컬스, 인크. 약물 조합체
BR112018000054A2 (pt) 2015-07-02 2018-09-04 Otsuka Pharmaceutical Co., Ltd. composições farmacêuticas liofilizadas
KR20200035438A (ko) 2017-08-03 2020-04-03 오쓰까 세이야꾸 가부시키가이샤 약물 화합물 및 이의 정제 방법

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