Treatment for inhibiting neoplastic lesions
First Claim
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1. A composition comprising one or more compound of the present invention, their derivatives, metabolites, analogues and/or mimic molecules with pharmaceutical acceptable additives, diluents, carriers, excipients and pharmaceutical salts thereof.
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Abstract
The invention discloses the use of incensole and/or furanogermacrens, derivatives metabolites and precursors thereof in the treatment of neoplasia, particularly resistant neoplasia and immunodysregulatory disorders. These compounds can be administered alone or in combination with conventional chemotherapeutic, anti-rival, anti-parasite agents, radiation and/or surgery.
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Citations
69 Claims
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1. A composition comprising one or more compound of the present invention, their derivatives, metabolites, analogues and/or mimic molecules with pharmaceutical acceptable additives, diluents, carriers, excipients and pharmaceutical salts thereof.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69)
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2. The composition as claimed in claim 1, wherein the compounds of the present invention are selected from the group comprising:
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3. The composition as claimed in claims 1 or 2, wherein the compounds of the present invention are selected from the group comprising:
- incensole, incensole acetate, incensole oxide, incensole oxide acetate, isoincensole, isoincensole acetate, isoincensole oxide, octyl acetate, octanol, terpinyl acetate, bornyl acetate, trans-ver-benol, verbenone, menthadien-7-ol, terpinen-4-ol, trans-pinocarveol, carvone, borneol, farnesol, farnesene, β
-caryophyllene, humulene, β
-cadinene, bergamotone, β
-guaiene, β
-ylangene, β
-bourbonene, α
-copaene, terpinene, myrcene, ρ
-cyrnene, α
- and β
-phellandrene, α
-thujene, cembrane-A, isocembrane, cembranol, cembranoids, cembranoid alcohols, furanogermacrens, furanogermacrene, germacrene, elemane, cadinene, guaiane, oplopane, eudsmane, echinodol, α
-santalene, α
-bisabolene, furanodiene, β
-santalene, β
-bergamotene, β
-farnesene, β
-bisabolene, SKB4, their derivatives, metabolites, analogues and/or mimic molecules with pharmaceutical acceptable additives, diluents, carriers and excipients and pharmaceutically acceptable salts thereof.
- incensole, incensole acetate, incensole oxide, incensole oxide acetate, isoincensole, isoincensole acetate, isoincensole oxide, octyl acetate, octanol, terpinyl acetate, bornyl acetate, trans-ver-benol, verbenone, menthadien-7-ol, terpinen-4-ol, trans-pinocarveol, carvone, borneol, farnesol, farnesene, β
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4. The composition as claimed in any preceding claims, wherein the compounds of the present invention are selected from the group comprising at least one of:
- incensole, incensole acetate, incensole oxide, incensole oxide acetate, isoincensole, isoincensole acetate, isoincensole oxide, and/or at least one of the furanosesquiterpene fumogermacrens, their derivatives, metabolites, analogues and/or mimic molecules with pharmaceutical acceptable additives, diluents, carriers and excipients and pharmaceutically acceptable salts thereof.
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5. A pharmaceutical formulation comprising a composition as claimed in any of claims 1 to 4 and a pharmaceutically acceptable carrier thereof.
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6. The pharmaceutical formulation as claimed in claim 5, wherein the pharmaceutical carrier is selected from the group comprising cyclodextrin, alpha-cyclodextrin, beta-cyclodextrin, (beta-hydroxypropylcyclodextrin) gamma-cyclodextrin and vitamin E oil.
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7. The use of a pharmaceutical formulation for the manufacture of a medicament for treatment of a mammal suffering from a neoplasia comprising a pharmaceutical formulation as claimed in claims 1 to 6.
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8. The use of a pharmaceutical formulation as claimed in any of the preceding claims, wherein the pharmaceutical formulation further includes at least one conventional chemotherapeutic agent.
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9. The use of a pharmaceutical formulation as claimed in claim 7, wherein the chemotherapeutic agent is selected from the group comprising flutamide and luprolide, antioestrogens, such as tamoxifen, antimetabolites and cytotoxic agents, such as daunorubicin, flourouracil, floxuridine, interferon alpha, methotrexate, plicamycin, mecaptopurine, thioguanine, adramycin, carmustine, lomustine, cytarabine, cyclophosphamide, doxorubicin, estramustine, altretamine, hydroxyurea, ifosfamide, procarbazine, mutamycin, busulfan, mitoxantrone, carboplatin, cisplatin, streptozooin, bleomycin, dactinomycin and idamycin, hormones such as, medroxyprogesterone, estramustine, ethinyl oestradiol, oestradiol, leuprolide, megestrol, octreotide, diethylstilbestrol, chlorotrianisene, etoposide, podophyllotoxin, and goserelin, nitrogen mustard derivatives such as, melphalan, chlorambucil, methlorethamine and thiotepa, steroids such as, betamethazone, and other antineoplastic agents such as live Mycobacterium bovis, dicarbazine, asparaginase, leucovoribn, mitotane, vincristine, vinblastine and texotere, cyclophosphamide, adriamycin, 5-flourouracil, hexamethylmelamine, Acivicin;
- Aclarubicin;
Acodazole Hydrochloride;
AcrQnine;
Adozelesin;
Aldesleukin;
Altretamine;
Ambomycin;
Ametantrone Acetate;
Aminoglutethimide;
Amsacrine;
Anastrozole;
Anthramycin;
Asparaginase;
Asperlin;
Azacitidine;
Azptepa;
Azotomycin;
Batimastat;
Benzodepa;
Bicalutamide;
Bisantrene Hydrochloride;
Bisnafide Dimesylate;
Bizelesin;
Bleomycin Sulfate;
Brequinar Sodium;
Bropirimine;
Busulfan;
Cactinomycin;
Calusterone;
Caracemide;
Carbetimer;
Carboplatin;
Carmustine;
Carubicin Hydrochloride;
Carzelesin;
Cedefingol;
Chlorambucil;
Cirolemycin;
Cisplatin;
Cladribino;
Crisnatol Mesylate;
Cyclophosphamide;
Cytarabine;
Dacarbazine;
Dactinomycin;
Daunorubicin Hydrochloride;
Decitabine;
Dexormaplatin;
Dezaguanine;
Dezaguanine Mesylate;
Diaziquone;
Docetaxel;
Doxorubicin;
Doxorubicin Hydrochloride;
Droloxifene;
Droloxifene Citrate;
Dromostanolone Propionate;
Duazomycin, Edatrexate;
Eflomithine Hydrochloride;
Elsamitrucin;
Enloplatin;
Enpromate;
Epipropidine, Epirubicin Hydrochloride;
Erbulozole;
Esorubicin Hydrochloride;
Estramustine;
Estramustine Phosphate Sodium;
Etanidazole;
Ethiodized Oil I 131;
Etoposide;
Etoposide Phosphate;
Etoprine;
Fadrozole Hydrochloride;
Fazarabine;
Fenretinide;
Floxuridine;
Fludarabine Phosphate;
Fluorouracil;
Flurocitabine;
Fosquidone;
Fostriecin Sodium;
Gemcitabine;
Gemcitabine Hydrochloride;
Gold Au 198;
Hydroxyurea;
Idarubicin Hydrochloride;
Ifosfamide;
Ilmofosine;
Interferon Alfa-2a;
Interferon Alfa-2b;
Interferon Alfa-n1;
Interferon Alfa-n3;
Interferon Beta-Ia;
Interferon Gamma-Ib;
Iproplatin;
Irinotecan Hydrochloride;
Lanreotide Acetate;
Letrozole;
Leuprolide Acetate;
Liarozole Hydrochloride;
Lometrexol Sodium;
Lomustine;
Losoxantrone Hydrochloride;
Masoprocol;
Maytansine;
Mechlorethamine Hydrochloride;
Megestrol Acetate;
Melengestrol Acetate;
Melphalan;
Menogaril;
Mercaptopurine;
Methotrexate;
Methotrexate Sodium;
Metoprine;
Meturedepa;
Mitindomide;
Mitocarcin;
Mitocromin;
Mitogillin;
Mitomalcin;
Mitomycin;
Mitosper;
Mitotane;
Mitoxantrone Hydrochloride;
Mycophenolic Acid;
Nocodazole;
Nogalamycin;
Ormaplatin;
Oxisuran;
Paclitaxel;
Pegaspargase;
Peliomycin;
Pentamustine;
Peplomycin Sulfate;
Perfosfamide;
Pipobroman;
Piposulfan;
Piroxantrone Hydrochloride;
Plicamycin;
Plomestane;
Porfimer Sodium;
Porfiromycin;
Prednimustine;
Procarbazine Hydrochloride;
Puromycin;
Puromycin Hydrochloride;
Pyrazofurin;
Riboprine;
Rogletimide;
Safrngol;
Safingol Hydrochloride;
Semustine;
Simtrazene;
Sparfosate Sodium;
Sparsomycin;
Spirogermanium Hydrochloride;
Spiromustine;
Spiroplatin;
Streptonigrin;
Streptozocin;
Strontium Chloride Sr 89;
Sulofenur;
Talisomycin;
Taxane;
Taxoid;
Tecogalan Sodium;
Tegafur;
Teloxantrone Hydrochloride;
Temoporfin;
Teniposide;
Teroxirone;
Testolactone;
Thiamiprine;
Thioguanine;
Thiotepa;
Tiazofurin;
Tirapazamine;
Topotecan Hydrochloride;
Toremifene Citrate;
Trestolone Acetate;
Triciribine Phosphate;
Trimetrexate;
Trimetrexate Glucuronate;
Triptorelin;
Tubulozole Hydrochloride;
Uracil Mustard;
Urodepa;
Vapreotide;
Verleporfin;
Vinblastine Sulfate;
Vincristine Sulfate;
Vindesine;
Vindesine Sulfate;
Vinepidine Sulfate;
Vinglycinate Sulfate;
Vinleurosine Sulfate;
Vinorelbine Tartrate;
Vinrosidine Sulfate;
Vinzolidine Sulfate;
Vorozole;
Zeniplatin;
Zinostatin;
Zorubicin Hydrochloride, 20-epi-1,25 dihydroxyvitamin D3;
5-ethynyluracil;
abiraterone;
aclarubicin;
acylfulvene;
adecypenol;
adozelesin;
aldesleukin;
ALL-TK antagonists;
altretamine;
ambamustine;
amidox;
amifostine;
aminolevulinic acid;
amrubicin;
atrsacrine;
anagrelide;
anastrozole; and
rographolide;
angiogenesis inhibitors;
antagonist D;
antagonist G;
DHEA;
bromineepiandrosterone;
epiandrosterone;
antarelix;
anti-dorselizing morphogenetic protein-1;
antiandrogen, prostatic carcinoma;
antiestrogen;
antineoplaston;
antisense oligonucleotides;
aphidicolin glycinate;
apoptosis gene modulators;
apoptosis regulators;
apurinic acid;
ara-CDP-DL-PTBA;
arginine deaminase;
asulacrine;
atamestane;
atrimustine;
axinastatin 1;
axinastatin 2;
axinastatin 3;
azasetron;
azatoxin;
azatyrosine;
baccatin III derivatives;
balanol;
batimastat;
BCR/ABL antagonists;
benzochlorins;
benzoylstaurosporine;
beta lactam derivatives;
beta-alethine;
betaclamycin B;
betulinic acid;
bFGF inhibitor;
bicalutamide;
bisantrene;
bisaziridinylspermine;
bisnafide;
bistratene A;
bizelesin;
breflate;
bropirimine;
budotitane;
buthionine sulfoximine;
calcipotriol;
calphostin C;
camptothecin derivatives;
canarypox IL-2;
capedtabine;
carboxamide-amino-triazole;
carboxyamidotriazole;
CaRest M3;
CARN 700;
cartilage derived inhibitor;
carzelesin;
casein kinase inhibitors (ICOS);
castanospermine;
cecropin B;
cetrorelix;
chlorins;
chloroquinoxaline sulfonamide;
cicaprost;
cis-porphyrin;
cladribine;
clomifene analogues;
clotrimazole;
collismycin A;
collismycin B;
combretastatin A4;
combretastatin analogue;
conagenin;
crambescidin 816;
crisnatol;
cryptophycin 8;
cryptophycin A derivatives;
curacin A;
cyclopentanthraquinones;
cycloplatam;
cypemycin;
cytarabine ocfosfate;
cytolytic factor;
cytostatin;
dacliximab;
decitabine;
dehydrodidemnin B;
deslorelin;
dexifosfamide;
dexrmzoxane;
dexverapamil;
diaziquorie;
didemnin 13;
didox;
diethylnorspermine;
dihydro-5-azacytidine;
dihydrotaxol, 9-;
dioxamycin;
diphenyl spiromustine;
docosanol;
dolasetron;
doxifluridine;
droloxifene;
dronabinol;
duocannycin SA;
ebselen;
ecorustine;
edelfosine;
edrocolomab;
eflornithine;
elemene;
emitefur;
epirubicin;
epristeride;
estramustine analogue;
estrogen agonists;
estrogen antagonists;
etanidazole;
etoposide phosphate;
exemestane;
fadrozole;
fazarabine;
fenretinide;
fligrastim;
finasteride;
flavopiridol;
flezelastine;
fluasterone;
fludarabine;
fluorodaunorunicin hydrochloride;
forfenimex;
formestane;
fostriecin;
fotemustine;
gadolinium texaphyrin;
gallium nitrate;
galocitabine;
ganirelix;
gelatinase inhibitors;
gemcitabine;
glutathione inhibitors;
hepsulfam;
heregulin;
hexamethylene bisacetamide;
hypericin;
ibandronic acid;
idarubicin;
idoxifene;
idramantone;
ilmofosine;
ilomastat;
imidazoacridones;
imiquimod;
immunostimulant peptides;
insulin-like growth factor-1 receptor inhibitor;
interferon agonists;
interferons;
interleukins;
iobenguane;
iododoxorubicin;
ipomeanol, 4-;
irinolecan;
iroplact;
irsogladine;
isobengazole;
isohomohalicondrin B;
itasetron;
jasplakinolide;
kahalalide F;
lamellarin-N triacetate;
lanreotide;
leinamycin;
lenograstim;
lentinan sulfate;
leptolstatin;
letrozole;
leukemia inhibiting factor;
leukocyte alpha interferon;
leuprolide+estrogen+progesterone;
leuprorelin;
levamisole;
liarozole;
linear polyamine analogue;
lipophilic disaccharide peptide;
lipophilic platinum compounds;
lissoclinamide 7;
lobaplatin;
lombricine;
lometrexol;
lonidamine;
losoxantrone;
lovastatin;
loxoribine;
lurtotecan;
lutetlum texaphyrin;
lysofylline;
lytic peptides;
maitansine;
mannostatin A;
marimastat;
masoprocol;
maspin;
matrilysin inhibitors;
matrix metalloproteinase inhibitors;
menogaril;
merbarone;
meterelin;
methioninase;
metoclopramide;
MIF inhibitor;
mifepristone;
miltefosine;
mirimostim;
mismatched double stranded RNA;
mitoguazone;
mitolactol;
mitomycin analogues;
mitonafide;
mitotoxin fibroblast growth factor-saporin;
mitoxantrone;
mofarotene;
molgramostim;
monoclonal antibody, human chorionic gonadotrophin;
monophosphoryl lipid A+myobacterium cell wall sk;
mopidamol;
multiple drug resistance genie inhibitor;
multiple tumor suppressor 1-based therapy;
mustard anticancer agent;
mycaperoxide B;
mycobacterial cell wall extract;
myriaporone;
N-acetyldinaline;
N-substituted benzamides;
nafarelin;
nagrestip;
naloxone+pentazocine;
napavin;
naphterpin;
nartograstim;
nedaplatin;
nemorubicin;
neridronic acid;
neutral endopeptidase;
nilutamide;
nisamycin;
nitric oxide modulators;
nitroxide antioxidant;
nitrullyn;
O6-benzylguanine;
octreotide;
okicenone;
oligonucleotides;
onapristone;
ondansetron;
ondansetron;
oracin;
oral cytokine inducer;
ormaplatin;
osaterone;
oxaliplatin;
oxaunomycin;
paclitaxel analogues;
paclitaxel derivatives;
palauamine;
palmitoylrizoxin;
pamidronic acid;
panaxytriol;
panomifene;
parabactin;
pazelliptine;
pegaspargase;
peldesine;
pentosan polysulfate sodium;
pentostatin;
pentrozole;
perflubron;
perfosfamide;
perillyl alcohol;
phenazinomycin;
phenylacetate;
phosphatase inhibitors;
picibanil;
pilocarpine hydrochloride;
pirarubicin;
piritrexim;
placetin A;
placetin B;
plasminogen activator inhibitor, platinum complex;
platinum compounds;
platinum-triamine complex;
porfimer sodium;
porfiromycin;
propyl bis-acridone, prostaglandin J2;
proteasome inhibitors;
protein A-based immune modulator;
protein kinase C inhibitor;
protein kinase C inhibitors, microalgal;
protein tyrosine phosphatase inhibitors;
purine nucleoside phosphorylase inhibitors;
purpurins;
pyrazoloacridine;
pyridoxylated hemoglobin polyoxyethylene conjugate;
raf antagonists;
raltitrexed;
ramosetron;
ras farnesyl protein transferase inhibitors;
ras inhibitors;
ras-GAP inhibitor;
retelliptine demethylated;
rhenium Re 186 etidronate;
rhizoxin;
ribozymes;
RII retinamide;
rogletimide;
rohitumine;
romurtide;
roquinimex;
rubiginone B1;
ruboxyl;
safingol;
saintopin;
SarCNU;
sarcophytol A;
sargramostim;
Sdi 1 mimetics;
semustine;
senescence derived inhibitor 1;
sense oligonucleotides;
signal transduction inhibitors;
signal transduction modulators;
single chain antigen binding protein;
sizofiran;
sobuzoxane;
sodium borocaptate;
sodium phenylacetate;
solverol;
somatomedin binding protein;
sonermin;
sparfosic acid;
splcamycin D;
spiromustine;
splenopentin;
spongistatin 1;
squalamine;
stem cell inhibitor;
stem-cell division inhibitors;
stipiamide;
stromelysin inhibitors;
sulfmosine;
superactive vasoactive intestinal peptide antagonist;
suradista;
suramin;
swainsonine;
synthetic glycosaminoglycans;
tallimustine;
tamoxifen methiodide;
tauromustine;
tazarotene;
tecogalan sodium;
tegafur, tellurapyrylium;
telomerase inhibitors;
telnoporfin;
ternozolomide;
teniposide;
tetrachlorodecaoxide;
tetrazomine;
thallblastine;
thalidomide;
thiocoraline;
thrombopoietin;
thrombopoietin mimetic;
thymalfasin;
thymopoietin receptor agonist;
thymotrinan;
thyroid stimulating hormone;
tin ethyl otiopurpurin;
tirapazamine;
titanocene dichloride;
topotecan;
topsentin;
toremifene;
totipotent stem cell factor;
translation inhibitors;
tretinoin;
triacetyluridine;
triciribine;
trimetrexate;
triptorelin;
tropisetron;
turosteride;
tyrosine kinase inhibitors;
tyrphostins;
UBC inhibitors;
ubenimex;
urogenital sinus-derived growth inhibitory factor;
urokinase receptor antagonists;
vapreotide;
variolin B;
vector system, erythrocyte gene therapy;
velaresol;
venom, anti-venom, veramine;
verdins;
verteporfin;
vinorelbine;
vinxaltine;
vitaxin;
vorozole;
zanoterone;
zeniplatin;
zilascorb;
zinostatin stimalamer, immunostimulating drugs or therapeutic agents, their metabolites, salts and derivatives thereof.
- Aclarubicin;
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10. The use of a pharmaceutical formulation as claimed in claims 7 to 9, wherein the pharmaceutical formulation is administered in combination with radiation treatment.
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11. The use of a pharmaceutical formulation as claimed in claims 7 to 10, wherein the pharmaceutical formulation is administered in combination with surgery.
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12. The use of a pharmaceutical formulation as claimed in claims 7 to 11, wherein the neoplasia is a precancerous lesion including syndromes represented by abnormal neoplastic and/or dysplastic, changes of tissue comprising precancerous growths in colonic, breast, renal, central nervous, gastric, or lung tissues, or conditions such as dysplastic nevus syndrome, a precursor to malignant melanoma of the skin, dysplastic nevus syndromes, polyposis syndromes, colonic polyps, precancerous lesions of the cervix (i.e., cervical dysplasia), prostatic dysplasia, bronchial dysplasia, breast, bladder and/or skin and related conditions (e.g., actinic keratosis), whether the lesions are clinically identifiable or not.
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13. The use of a pharmaceutical formulation as claimed in claims 7 to 12, wherein the neoplasia is prostate cancer, colon cancer, small cell lung cancer, large cell lung cancer, lung adenocarcinoma, epidermoid lung cancer, melanoma (including amelanotic subtypes), renal cell carcinoma, gastric carcinoma, cancers of the central nervous system including brain tumours, neuroblastomas, gastric carcinoma, breast cancer, ovarian cancer, testicular cancer, lymphoma and leukaemia, oesophageal cancer, stomach cancer, liver cancers, prostate cancer, cervical cancer, adrenal cancer, oral or mucosal cancer, bladder cancer, pancreatic cancer, lymphoma, Hodgkins disease, sarcomas, Hematopoeitic cell cancers such as B cell leukaemia/lymphomas, myelomas, T-cell leukemias/lymphomas, small cell leukemias/lymphomas, null cell, sezary, monocytic, myelomonocytic and Hairy cell leukemias.
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14. The use of a pharmaceutical formulation as claimed in claims 7 to 13, wherein the neoplasia is in the form of a tumour comprising an epidermoid and myeloid tumour, acute or chronic, nonsmall cell, squamous or solid.
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15. The use of a pharmaceutical formulation as claimed in claims 7 to 14, wherein the composition is micronized.
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16. The use of a pharmaceutical formulation as claimed in claims 7 to 15, wherein the pharmaceutical formulation has an enteric coating.
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17. The use of a pharmaceutical formulation as claimed in claim 16, wherein the enteric coating is made of a polymer or copolymer.
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18. The use of a pharmaceutical formulation as claimed in claim 17, wherein the polymer or copolymer is selected from the group consisting of poly(lactic-glycolic acid) polyester, cellulose acetate phthalate, hydroxypropyl-methyl cellulose phthalate poly(butyl methacrylate), (2-dimethyl aminoethyl) methacrylate, and methyl methacrylate.
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19. The use of a pharmaceutical formulation as claimed in claims 7 to 18, wherein, the pharmaceutical formulation is administered enterally, parenterally, topically, orally, sub-lingually, rectally, nasally or vaginally.
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20. The use of a pharmaceutical formulation as claimed in claims 7 to 19, wherein the composition is formulated into liposomes or carbohydrate vehicles.
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21. The use of a pharmaceutical formulation as claimed in claim 20, wherein the liposomes or carbohydrate vehicles are specifically targeted to tumours by covalently attaching a monoclonal antibody directed to a tumour-associated antigen.
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22. The use of a pharmaceutical formulation as claimed in claims 7 to 21, wherein the pharmaceutical formulation is administered intermittently.
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23. The use of a pharmaceutical formulation as claimed in claims 7 to 22, wherein the pharmaceutical formulation is a unit dose that comprises 5-500 mg of active ingredient consisting of at least one compound of the present invention.
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24. The use of a pharmaceutical formulation as claimed in claims 7 to 23, wherein the pharmaceutical formulation is administered to a mammal.
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25. The use of a pharmaceutical formulation as claimed in claim 24, wherein said mammal is a neonate and said administering is effected prior to delivery of said neonate and/or during delivery of said neonate.
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26. The use of a pharmaceutical formulation as claimed in claims 7 to 25, wherein said compounds of the present invention acts as a prodrug.
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27. The use of a pharmaceutical formulation for the manufacture of a medicament for treatment of a mammal suffering from an immunodysregulatory condition comprising a composition as claimed in claims 1 to 6, to a subject.
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28. The use of a pharmaceutical formulation as claimed in claim 27, wherein the immunodysregulation condition is caused by a viral infection, intracellular bacterial infection, extracellular bacterial infection, fungal infection, yeast infection, extracellular parasite infection, intracellular parasite infection, protozoan parasite, multicellular parasite, autoimmune disease, immunosuppressive therapy, chemotherapy, anti-infective agent therapy, wound, burn, the presence of an immunosuppressive molecule, gastrointestinal irritation or any combination of the foregoing is selected from (a) a DNA virus infection or an RNA virus(b) a parasite infection, a Trypanosoma, Plasmodium, Cryptosporidium, Entamoeba, Balantidium, Leishmania, Pneumocystis, Trichomoniasis or Toxoplasma Infection, wherein the Trypanosoma, Plasmodium, Cryptosporidium, Entamoeba, Balantidium, Leishmania, Pneumocystis, Trichomoniasis or Toxoplasma infection is selected from but not limited to Tryponosoma cruzi, Tryponosoma brucei, Trypanosoma gambiense, Trypanosoma rhodesiense, Plasmodium falciparum;
- Plasmodium vivax, Plasmodium malariae, Plasmodium ovale;
Plasmodium berghei, Entamoeba histolytica, Balantidium coli, Leishmania brazillenis, Leishmania mexicana, Leishmania donovani, Leishmania tropica, Pneumocystis carinii, Trichomoniasis vaginalis, and Toxoplasma gondii (c) a mycoplasma infection, a Listeria infection or a Mycobacterium infection;
(d) a Streptococcus infection, a Staphylococcus infection, a Vibrio infection, a Salmonella infection;
a Shigella infection, an enterotoxigenic, enteropathogenic, enteroinvasive or enterohemorrhagic E. coli infection, a Yersinia infection, a Campylobacter infection, a Pseudomonas infection, a Borrelia infection, a Legionella infection and a Haemophilus infection;
(e) pulmonary Aspergillosis, mucosal or oropharyngealcandidiasis and juvenile paracoccidiomyosis, (f) a Candida infection and a Cryptococcus infection;
(g) systemic lupus erythematosis, arthritis, asthma, and diabetes (h) adriamycin treatment, cisplatin treatment, mitomycin C treatment, amphoteracin B treatment;
(i) a gamma-radiation treatment;
(j) nucleoside analog treatment for viral infection or for cancer, (k) surgical and accidental wounds, septic shock caused by surgery;
(l) cyclosporin treatment and corticosteroid treatment;
(m) irritable bowel treatment, Crohn'"'"'s disease, wasting syndrome, cachexia, Motor Neuron disease, Multiple Sclerosis, inflammatory bowel disease, respiratory distress syndrome, chronic diarrhoea;
(n) cancer, (o) cirrhoisis;
(p) gram positive multi-drug resistant bacteria or (q) any combination of (a) through (p).
- Plasmodium vivax, Plasmodium malariae, Plasmodium ovale;
-
29. The use of a pharmaceutical formulation as claimed in claim 28, wherein the DNA virus infection or the RNA virus infection is selected from a retrovirus infection, a togavirus infection, a flavivirus infection, a rubivirus infection, a pestivirus infection, a lipia envelope virus infection, a filovirus, a picornavirus infection, a rhinovirus infection, a coronavirus infection, a respiratory syncytial virus infection, a poliovirus infection, a parainfluenza virus infection, influenza virus infection, hantavirus, adeno-associated virus, measles virus, poxvirus, filovirus, human papilloma virus and animal papilloma virus infection.
-
30. The use of a pharmaceutical formulation as claimed in claims 27 to 29, wherein the composition further includes at least one conventional chemotherapeutic agent.
-
31. The pharmaceutical formulation as claimed in claim 30, wherein the chemotherapeutic agent is selected from the group comprising flutamide and luprolide, antioestrogens, such as tamoxifen, antimetabolites and cytotoxic agents, such as daunorubicin, flourouracil, floxuridine, interferon alpha, methotrexate, plicamycin, mecaptopurine, thioguanine, adramycin, carmustine, lomustine, cytarabine, cyclophosphamide, doxorubicin, estramustine, altretamine, hydroxyurea, ifosfamide, procarbazine, mutamycin, busulfan, mitoxantrone, carboplatin, cisplatin, streptozocin, bleomycin, dactinomycin and idamycin, hormones such as, medroxyprogesterone, estramustine, ethinyl oestradiol, oestradiol, leuprolide, megestrol, octreotide, diethylstilbestrol, chlorotrianisene, etoposide, podophyllotoxin, and goserelin, nitrogen mustard derivatives such as, melphalan, chlorambucil, methlorethamine and thiotepa, steroids such as, betamethasone, and other antineoplastic agents such as live Mycobacterium bovis, dicarbazine, asparaginase, laucovoribn, mitotone, vincristine, vinblastine and texotere, cyclophosphamide, adriamycin, 5-flourouracil, hexamethylmelamine, Acivicin;
- Aclarubicin;
Acodazole Hydrochloride;
AcrQnine;
Adozelesin;
Aldesleukin;
Altretamine;
Ambomycin;
Ametantrone Acetate;
Aminoglutethimide;
Amsacrine;
Anastrozole;
Anthramycin;
Asparaginase;
Asperlin;
Azacitidine;
Azetepa;
Azotomycin;
Batimastat;
Benzodepa;
Bicalutamide;
Bisantrene Hydrochloride;
Bisnafide Dimesylate;
Bizelesin;
Bleomycin Sulfate;
Brequinar Sodium;
Bropirimine;
Busulfan;
Cactinomycin;
Calusterone;
Caracemide;
Carbetimer;
Carboplatin;
Carmustine;
Carubicin Hydrochloride;
Carzelesin;
Cedefingol;
Chlorambucil;
Cirolemycin;
Cisplatin;
Cladribine;
Crisnatol Mesylate;
Cyclophosphamide;
Cytarabine;
Dacarbazine;
Dactinomycin;
Daunonibicin Hydrochloride;
Decitabine;
Dexormaplatin;
Dezaguanine;
Dezaguanine Mesylate;
Diaziquone;
Docetaxol;
Doxorubicin;
Doxorubicin Hydrochloride;
Droloxifene;
Droloxifene Citrate;
Dromostanolone Propionate;
Duazomycin;
Edatrexate;
Eflomithine Hydrochloride;
Elsamitrucin;
Enloplatin;
Enpromate;
Epipropidine;
Epirubicin Hydrochloride;
Erbulozole;
Esorubicin Hydrochloride;
Estramustine;
Estramustine Phosphate Sodium;
Etanidazole;
Ethiodized Oil I 131;
Etoposide;
Etoposide Phosphate;
Etoprine;
Fadrozole Hydrochloride;
Fazarabine;
Fenretinide;
Floxuridine;
Fludirabine Phosphate;
Fluouracil;
Flurocitabine;
Fosquidone;
Fostriecin Sodium;
Gemcitabine;
Gemcitabine Hydrochloride;
Gold Au 198;
Hydroxyurea;
Idarubicin Hydrochloride;
Ifosfamide;
Ilmofosine;
Interferon Alfa-2a;
Interferon Alfa-2b;
Interferon Alfa-n1;
Interferon Alfa-n3;
Interferon Beta-Ia;
Interferon Gamma-Ib;
Iproplatin;
Irinotecan Hydrochloride;
Lanreotide Acetate;
Letrozole;
Leuprolide Acetate;
Liarozole Hydrochloride;
Lometrexol Sodium;
Lomustine;
Losxantrone Hydrochloride;
Masoprocol;
Maytansine;
Mechlorethamine Hydrochloride;
Megestrol Acetate;
Melengestrol Acetate;
Melphalan;
Menogaril;
Mercaptopurine;
Methotrexate;
Methotrexate Sodium;
Metoprine;
Meturedepa;
Mitindomide;
Mitocarcin;
Mitocromin;
Mitogillin;
Mitomalcin;
Mitomycin;
Mitosper;
Mitotane;
Mitoxantrone Hydrochloride;
Mycophenolic Acid;
Nocodozole;
Nogalamycin;
Ormaplatin;
Oxisuran;
Paclitaxel;
Pegaspargase;
Peliomycin;
Pentamustine;
Peplomycin Sulfate;
Perfosfamide;
Pipobroman;
Piposulfan;
Piroxantrone Hydrochloride;
Plicamycin;
Plomestane;
Porfimer Sodium;
Porfiromycin;
Prednimustine;
Procarbazine Hydrochloride;
Puromycin;
Puromycin Hydrochloride;
Pyrazofurin;
Riboprine;
Rogletimide;
Safrngol;
Safingol Hydrochloride;
Semustine;
Simtrazene;
Sparfosate Sodium;
Sparsomycin;
Spirogermanium Hydrochloride;
Spiromustine;
Spiroplatin;
Streptonigrin;
Streptozocin;
Strontium Chloride Sr 89;
Sulofenur;
Tallsomycin;
Taxane;
Taxoid;
Tecogalan Sodium;
Tegafur;
Teloxantrone Hydrochloride;
Temoporfin;
Teniposide;
Teroxirone;
Testolactone;
Thiamiprine;
Thioguanine;
Thiotepa;
Tiazofurin;
Tirapazamine;
Topotecan Hydrochloride;
Toremifene Citrate;
Trestolone Acetate;
Triciribine Phosphate;
Trimetrexate;
Trimetrexate Glucuronate;
Triptorein;
Tubulozole Hydrochloride;
Uracil Mustard;
Uredepa, Vapreotide;
Verteporfin;
Vinblastine Sulfate;
Vincristine Sulfate;
Vindesine;
Vindesine Sulfate;
Vinapidine Sulfate;
Vinglycinate Sulfate;
Vinieurosine Sulfate;
Vinorelbine Tartrate;
Vinrosidine Sulfate;
Vinzolidine Sulfate;
Vorozole;
Zeniplatin;
Zinostatin;
Zorubicin Hydrochloride, 20-epi-1,25 dihydroxyvitamin D3;
5-ethynyluracil;
abiraterone;
aclarubicin;
acylfulvene;
adecypenol;
adozesin;
aldesleukin;
ALL-TK antagonists;
altretemine;
ambamustine;
amidox;
amifostine;
aminolevulinic add;
amrubicin;
atrsacrine;
anagrelide;
anastrazole; and
rographoilde;
angiogenesis inhibitors;
antagonist D;
antagonist G;
DHEA, bromineepiandrosterone;
epiandrosterone;
antarelix;
anti-dorsalizing morphogenetic protein-1;
antiandrogen, prostatic carcinoma;
antiestrogen;
antineoplaston;
antisense oligonucleotides;
aphidicolin glycinate;
apoptosis gene modulators;
apoptosis regulators;
apurinic acid;
ara-CDP-DL-PTSA;
arginine deaminase;
asulacrine;
atamestane;
atrimustine;
axinastatin 1;
axinastatin 2;
axinastatin 3;
azasetron;
azatoxin;
azatyrosine;
baccatin III derivatives;
balanol;
batimastat;
BCR/ABL antagonists;
benzochlorins;
benzoylstaurosporine;
beta lactam derivatives;
beta-alethine;
betaclamycin B;
betulinic acid;
bFGF inhibitor;
bicalutamide;
bisantrene;
bisaziridinylspermine;
bisnafide;
bistratene A;
bizelesin;
breflate;
bropirimine;
budotitane;
buthionine sulfoximine;
calcipotriol;
calphostin C;
camptothecin derivatives;
canarypox IL-2;
capecitabine;
carboxamide-amino-triazole;
carboxyamidotriazole;
CaRest M3;
CARN 700;
cartilage derived inhibitor;
carzelesin;
casein kinase inhibitors (ICOS);
castanospermine;
cecropin B;
cetrorelix;
chlorins;
chloroquinoxaline sulfonamide;
cicaprost;
cis-porphyrin;
cladribine;
clomifene analogues;
clotrimazole;
collismycin A;
collismycin B;
combretastatin A4;
combretastatin analogue;
conagenin;
crambescidin 816;
crisnatol;
cryptophycin 8;
cryptophydn A derivatives;
curacin A;
cyclopentanthraquinones;
cycloplatam;
cypemycin;
cytarabine ocfosfate;
cytolytic factor;
cytostatin;
dacliximab;
decitabine;
dehydrodidemnin B;
deslorelin;
doxifosfamide;
dexrazoxane;
dexverapamil;
diaziquone;
didemnin B;
didox;
diethylnorspermine;
dihydro-5-azacytidine;
dihydrotaxol, 9;
dioxamycin;
diphenyl spiromustine;
docosanol;
dolasetron;
doxifluridine;
droloxifene;
dronabinol;
duocannycin SA;
ebselen;
ecomustine;
edelfosine;
edrecolomab;
eflornithine;
elemene;
emitefur, epirubicin;
epristeride;
estramustine analogue;
estrogen agonists;
estrogen antagonists;
etanidazole;
etoposide phosphate;
exemestane;
fadrozole;
fazarabine;
fenretinide;
filgrastim;
frnasteride;
flavopiridol;
flezelastine;
fluasterone;
fludarabine;
fluorodaunorunicin hydrochloride;
forfenimex;
formestane;
fostriecin;
fotemustine;
gadolinium texaphyrin;
gallium nitrate;
galocitabine;
ganirelix;
gelatinase inhibitors;
gemcitabine;
glutathione inhibitors;
hepsulfam;
heregulin;
hexamethylene bisacetamide;
hypericin;
ibandronic acid;
idarubicin;
idruxifene;
idramantone;
ilmofosine;
ilomastat;
imidazoacridones;
imiquimod;
immunostimulant peptides;
insulin-like growth factor-1 receptor inhibitor;
interferon agonists;
interferons;
interleukins;
iobenquane;
iododoxorubicin;
ipomeanol, 1-;
irinotecan;
iroplact;
irsogladine;
isobengazole;
isohomohalicondrin B;
itasetron;
jasplakinolide;
kahalalide F;
lamellarin-N triacetate;
lanreotide;
leinamycin;
lenograstim;
lentinan sulfate;
leptolstatin;
letrozole;
leukemia inhibiting factor;
leukocyte alpha interferon;
leuprolide+estrogen+progesterone;
leuprorelin;
levamisole;
liarozole;
linear polyamine analogue;
lipophilic disaccharide peptide;
lipophilic platinum compounds;
lissoclinamide 7;
lobaplatin;
lombricine;
lometrexol;
lonidamine;
losoxantrone;
lovastatin;
loxoribine;
lurtotecan;
lutetium texaphyrin;
lysofylline;
lytic peptides;
maitansine;
mannostatin A;
marimastat;
masoprocol;
maspin;
matrilysin inhibitors;
matrix metalloproteinase inhibitors;
menogaril;
merbarone;
meterelin;
methioninase;
metoclopramide;
MIF Inhibitor;
mirfepristone;
miltefosine;
mirimostim;
mismatched double stranded RNA;
mitoguazone;
mitolactol;
mitomycin analogues;
mitonafide;
mitotoxin fibroblast growth factor-saporin;
mitoxantrone;
mofarotene;
molgramostim;
monoclonal antibody, human chorionic gonedotrophin;
monophosphoryl lipid A+myobacterium cell wall sk;
mopidamol;
multiple drug resistance genie inhibitor;
multiple tumorsuppressor 1-based therapy;
mustard anticancer agent;
mycaperoxide B;
mycobacterial cell wall extract;
myriaporone;
N-acetyldinaline;
N-substituted benzamides;
nafarelin;
nagrestip;
naloxone+pentazocine;
napavin;
naphterpin;
nartograstim;
nedaplatin;
nemorubicin;
neridronic acid;
neutral endopeptidase;
nilutamide;
nisamycin;
nitric oxide modulators;
nitroxide antioxidant;
nitrullyn;
O6-benzylguanine;
octreotide;
okicenone;
oligonucleotides;
onapristone;
ondansetron, ondansetron;
oracin;
oral cytokine inducer;
ormaplatin;
osaterone;
oxaliplatin;
oxaunomycin;
paclitaxel analogues;
paclitaxel derivatives;
palauamine;
palmitoylrhizoxin;
pamidronic acid;
panaxytriol;
panomifene;
parabactin;
pazelliptine;
pegaspargase;
peldesine;
pentosan polysulfate sodium;
pentostatin;
pentrozole;
perflubron;
perfosfamide;
perlilyl alcohol;
phenazinomycin;
phenylacetate;
phosphatase inhibitors;
picibanil;
pilocarpine hydrochloride;
pirarubicin;
piritrexim;
placetin A;
placetin B;
plasminogen activator inhibitor;
platinum complex;
platinum compounds;
platinum-triamine complex;
porfimer sodium;
porfiromycin;
propyl bis-acridone;
prostaglandin J2;
proteasome inhibitors;
protein-based immune modulator;
protein kinase C inhibitor;
protein kinase C inhibitors, microalgal;
protein tyrosine phosphitase inhibitor;
purin nucleoside phosphorylase inhibitors;
purpurins;
pyrazoloacridine;
pyridoxylated hemoglobin polyoxyethylene conjugate;
raf antagonists;
raltitrexed;
ramosetron;
ras farnesyl protein transferase inhibitors;
ras inhibitors;
ras-GAP inhibitor;
retelliptine demethylated;
rhenium Re 186 etidronate;
rhizoxin;
ribozymes;
RII retinamide;
rogletimide;
rohitukine;
romurtide;
roquinimex;
rubiginone B1;
ruboxyl;
safingol;
saintopin;
SarCNU;
sarcophytol A;
sargramostim;
Sdi 1 mimetics;
semustine;
senescence derived inhibitor 1;
sense oligonucleotides;
signal transduction inhibitors;
signal transduction modulators;
single chain antigen binding protein;
sizofiran;
sobuzoxane;
sodium borocaptate;
sodium phenylacetate;
solverol;
somatomedin binding protein;
sonermin;
sparfosic acid;
spicamycin D;
spiromustine;
splenopentin;
spongistatin 1;
squalamine;
stem cell inhibitor;
stem-cell division inhibitors;
stipiamide;
stromelysin inhibitors;
sulfmosine;
superactive vasoactive intestinal peptide antagonist;
suradista;
suramin;
swainsonine;
synthetic glycosaminoglycans;
tallimustine;
tamoxifen methiodide;
tauromustine;
tazarotene;
tecogalan sodium;
tegafur;
tellurapyrylium;
telomerase inhibitors;
temoporfin;
temozolomide;
teniposide;
tetrachlorodecaoxide;
tetrazomine;
thaliblastine;
thalidomide;
thiocoraline;
thrombopoietin;
thrombopoietin mimetic;
thymalfasin;
thymopoietin receptor agonist;
thymotrinan;
thyroid stimulating hormone;
tin ethyl etiopurpurin;
tirapazamine;
titanocene dichloride;
topotecan;
topsentin;
toremifene;
totipotent stem cell factor;
translation inhibitors;
tretinoin;
triacetyluridine;
triciribine;
trimetrexate;
triptorelin;
tropisetron;
turosteride;
tyrosine kinase inhibitors;
tyrphostins;
UBC inhibitors;
ubenimex;
urogenal sinus-derived growth inhibitory factor;
urokinase receptor antagonists;
vapreotide;
variolin B;
vector system, erythrocyte gene therapy;
velaresol;
venom, anti-venom, veramine;
verdins;
verteporfin;
vinorelbine;
vinxaltine;
vitaxin;
vorozole;
zanoterone;
zeniplatin;
zilascorb;
zinostatin stimalamer, immunostimulating drugs or therapeutic agents, their metabolites, salts and derivatives thereof.
- Aclarubicin;
-
32. The use of a pharmaceutical formulation as claimed in claims 27 to 31, wherein the composition further includes at least one anti-viral agent.
-
33. The use of a pharmaceutical formulation as claimed in claim 32, wherein the anti-viral agents are selected from the group comprising nucleoside analogues (AZT;
- ddC;
ddl;
d4T;
3TC;
BW 1592;
PMEA/bis-POM PMEA;
dOTC;
DAPD);
non-nucleoside reverse transcriptase inhibitor (delavirdine;
DMP 266;
HBY097;
loviride;
nevirapine, emivirine;
AG1549;
PNU142721;
Calanolide A;
DPC961);
protease inhibitors (ABT-378;
ritonavir;
nelfinavir;
BW 141;
KNI-272;
indinavir;
saquinavir;
L-756,423;
DMP-450;
BMS-2326;
30);
ALX40-4C;
hydroxyurea;
lobucavir;
pentafuside;
T-1249;
PRO 542;
FP-21399;
AMD 3100;
HE-2000 and pepude T;
Abacavir, Acemannan;
Acyclovir;
Acyclovir Sodium;
Adefovir;
Alovudine;
Alvircept Sudotox;
Amantadine Hydrochloride;
Aranotin;
Arildone;
Atevirdine Mesylate;
Avridine;
Cidofovir;
Cipamfylline;
Coviracil;
Cytarabine Hydrochloride;
Delavirdine Mesylate;
Desciclovir, Didanosine;
Disoxaril;
Edoxudine;
Emivirine;
Emtricitabine;
Enviradene;
Enviroxime;
Epivir;
Famciclovir;
Famotine Hydrochloride;
Fiacitabine;
Fialuridine;
Fosarilate;
Foscarnet Sodium;
Fosfonet Sodium;
Ganciclovir, Ganciclovir Sodium;
Idoxuridine;
Indinavir;
Kethoxal;
Lamivudine;
Lobucavir;
Lodenosine;
Lopinavir, Memotine Hydrochloride;
Methisazone;
Nelfinavir;
Nevirapine;
Penciclovir;
Pirodavir;
Ribavirin;
Rimantadine Hydrochloride;
Saquinavir Mesylate;
Ritonavir;
Somantadine Hydrochloride;
Sorivudine;
Statolon;
Stavudine;
Tenofovir;
Tilorone Hydrochloride;
Trifluridine;
Valacyclovir Hydrochloride;
Vidarabine;
Vidarabine Phosphate;
Vidarabine Sodium Phosphate;
Tipranavir, Viroxime;
Zalcitabine;
Zidovudine;
Zinviroxime and Interferon.
- ddC;
-
34. The use of a pharmaceutical formulation as claimed in claims 27 to 33, wherein the composition further includes at least one anti-parasite agent.
-
35. The use of a pharmaceutical formulation as claimed in claim 34, wherein the anti-parasite agents are selected from the group comprising chloroquin, primaquine, mefloquine, pyrimethamine-sulfadoxone, atoraquone/dapsone;
- halofantrine;
artemisinin derivatives;
atoraquone+proguanol, co-artemether;
podophyllotoxin;
pentamidine, diloxanide furoate;
metronidazole, tindazole, tetracycline, quinacrine, stibogluconate, amphotericin B, quinine, doxycline, trimethoprim-sulfamethoxazole, metronidazole, nifurtimox, suramin, melarsoprol, benznidazole, their metabolites, salts derivatives or any other anti-parasitic agent thereof.
- halofantrine;
-
36. The use of a pharmaceutical formulation as claimed in claims 27 to 35, wherein the composition is micronized.
-
37. The use of a pharmaceutical formulation as claimed in claims 27 to 36, wherein the composition enhances endogenous hsp levels.
-
38. The use of a pharmaceutical formulation as claimed in claims 27 to 37, wherein the composition enhances endogenous precursor dendritic cell levels.
-
39. The use of a pharmaceutical formulation as claimed in claims 27 to 38, wherein the pharmaceutical formulation has an enteric coating.
-
40. The use of a pharmaceutical formulation as claimed in claim 39, wherein the enteric coating is made of a polymer or copolymer.
-
41. The use of a pharmaceutical formulation as claimed in claim 40 wherein the polymer or copolymer is selected from the group consisting of poly(lactic-glycolic acid) polyester, cellulose acetate phthalate, hydroxypropyl-methyl cellulose phthalate poly(butyl methacrylate), (2-dimethyl aminoethyl) methacrylate, and methyl methacrylate.
-
42. The use of a pharmaceutical formulation as claimed in claims 27 to 41, wherein the pharmaceutical formulation is administered enterally, parenterally, topically, orally, rectally, nasally or vaginally.
-
43. The use of a pharmaceutical formulation as claimed in claims 27 to 42, wherein the composition is formulated into liposomes or carbohydrate vehicles.
-
44. The use of a pharmaceutical formulation as claimed in claim 43, wherein the liposomes or carbohydrate vehicles are targeted to HIV infected cells by putting viral antibodies on its surface.
-
45. The use of a pharmaceutical formulation as claimed in claim 44, wherein the viral antibodies are directed to the HIV coat protein gp160 and/or gp120.
-
46. The use of a pharmaceutical formulation as claimed in claims 27 to 45, wherein the pharmaceutical formulation is administered intermittently.
-
47. The use of a pharmaceutical formulation as claimed in claims 27 to 46, wherein the pharmaceutical formulation is administered to a mammal.
-
48. The use of a pharmaceutical formulation as claimed in claim 47, wherein said mammal is a neonate and said administering is effected prior to delivery of said neonate and/or during delivery of said neonate.
-
49. The use of a pharmaceutical formulation as claimed in claims 27 to 48, wherein said compounds of the present invention acts as a prodrug.
-
50. The use of a pharmaceutical formulation for the manufacture of a medicament for sensitising a resistant neoplasia to subsequent therapy comprising administering to a patient in need thereof a therapeutically effective amount of composition as claimed in claims 1 to 6.
-
51. The use of a pharmaceutical formulation as claimed in claim 50, wherein the pharmaceutical formulation further includes at least one conventional chemotherapeutic agent.
-
52. The use of a pharmaceutical formulation as claimed in claim 51, wherein the chemotherapeutic agent is selected from the group comprising flutamide and luprolide, antiestrogens, such as tamoxifen;
- antimetabolites and cytotoxic agents, such as daunorubicin, flourouracil, floxuridine, interferon alpha, methotrexate, plicamycin, mecaptopurine, thioguanine, adramycin, carmustine, lomustine, cytarabine, cyclophosphamide, doxorubicin, estramustine, altretamine, hydroxyurea, ifosfamide, procarbazine, mutamycin, busulfan, mitoxantrone, carboplatin, cisplatin, streptozocin, bleomycin, dactinomycin and idamycin, hormones such as, medroxyprogesterone, estramustine, ethinyl oestradiol, oestradiol, leuprolide, megestrol, octreotide, diethylstilbestrol, chlorotrianisene, etoposide, podophyllotoxin, and goserelin, nitrogen mustard derivatives such as, melphalan, chlorambucil, methlorethamine and thiotepa, steroids such as, betamethasone, and other antineoplastic agents such as live Mycobacterium bovis, dicarbazine, asparaginase, leucovoribn, mitotane, vincristine, vinblastine and texotere, cydophosphamide, adriamycin, 5-flourouracil, hexamethylmelamine, Acivicin;
Aclarubicin;
Acodazole Hydrochloride;
AcrQnine;
Adozolesin;
Aldesloukin;
Altretamine;
Ambomycin;
Ametantrone Acetate;
Aminogluthimide;
Amsacrine;
Anastrozole;
Anthramycin;
Asparaginase;
Asperlin;
Azacitidine;
Azetepa;
Azotomycin;
Batimastat;
Benzodepa;
Bicalutamide;
Bisantrene Hydrochloride;
Bisnafide Dimesylate;
Bizelesin;
Bleomycin Sulfate;
Brequinar Sodium;
Bropirimine;
Busulfan;
Cactinomycin;
Calusterone;
Caracemide;
Carbetimer;
Carboplatin;
Carmustine;
Carubicin Hydrochloride;
Carzelesin;
Cedefingol;
Chlorambucil;
Cirolemycin;
Cisplatin;
Cladribine;
Crisnatol Mesylate;
Cyclophosphamide;
Cytarabine;
Dacarbazine;
Dactinomycin;
Daunorubicin Hydrochloride;
Decitabine;
Dexormaplatin;
Dezaguanine;
Dezaguanine Mesylate;
Diaziquone;
Docetaxel;
Doxorubicin;
Doxorubicin Hydrochloride;
Droloxifene;
Droloxifene Citrate;
Dromostanolone Propionate;
Duazomyrin;
Edatrexate;
Eflomithine Hydrochloride;
Elsamitrucin;
Enloplatin;
Enprorfate;
Epipropidine;
Epirubicin Hydrochloride;
Erbulozole;
Esorubicin Hydrochloride;
Estramustine;
Estramustine Phosphate Sodium;
Etanidazole;
Ethiodized Oil I 131;
Etoposide;
Etoposide Phosphate;
Etoprine;
Fadrozole Hydrochloride;
Fazarabine;
Fenretinide;
Floxuridine;
Fludarabine Phosphate;
Fluorouracil;
Flurocitabine;
Fosquidone;
Fostriecin Sodium;
Gemcitabine;
Gemcitabine Hydrochloride;
Gold Au 198;
Hydroxyurea;
Idarubicin Hydrochloride;
Ifosfamide;
Ilmofosine;
Interferon Alfa-2a;
Interferon Alfa-2b;
Interferon Alfa-n1;
Interferon Alfa-n3;
Interferon Beta-Ia;
Interferon Gamma-Ib;
Iproplatin;
Irinotecan Hydrochloride;
Lanreotide Acetate;
Letrozole;
Leuprolide Acetate;
Liarozole Hydrochloride;
Lometrexol Sodium;
Lomustine;
Losoxantrone Hydrochloride;
Masoprocol;
Maytansine;
Mechlorethamine Hydrochloride;
Megestrol Acetate;
Melengestrol Acetate;
Melphalan;
Menogaril;
Mercaptopurine;
Methotrexate;
Methotrexate Sodium;
Metoprine;
Meturedepa;
Mitindomide;
Mitocarcin;
Mitocromin;
Mitogillin;
Mitomalcin;
Mitomycin;
Mitosper;
Mitotane;
Mitoxantrone Hydrochloride;
Mycophenolic Acid;
Nocodazole;
Nogalamycin;
Ormaplatin;
Oxisuran;
Paclitaxel;
Pegaspargase;
Peliomycin;
Pentamustine;
Peplomycin Sulfate;
Perfosfamide;
Pipobroman;
Piposulfan;
Piroxantrone Hydrochloride;
Plicamycin;
Plomestane;
Porfimer Sodium;
Porfiromycin;
Prednimustine;
Procarbazine Hydrochloride;
Puromycin;
Puromycin Hydrochloride;
Pyrazofurin;
Riboprine;
Rogletimide;
Safingol;
Safingol Hydrochloride;
Semustine;
Simtrazene;
Sparfosate Sodium;
Sparsomycin;
Spirogermanium Hydrochloride;
Spiromustine;
Spiroplatin;
Streptonigrin;
Streptozocin;
Strontium Chloride Sr 89;
Sulofenur;
Talisomycin;
Taxane;
Taxoid;
Tecogalan Sodium;
Tegafur;
Teloxantrone Hydrochloride;
Temoporfin;
Teniposide;
Teroxirono;
Testolactone;
Thiamiprine;
Thioguanine;
Thiotepa;
Tiazofurin;
Tirapazamine;
Topotecan Hydrochloride;
Toremifene Citrate;
Trestolone Acetate;
Triciribine Phosphate;
Trimetrexate;
Trimetrexate Glucuronate;
Triptorelin;
Tubulozole Hydrochloride;
Uracil Mustard;
Uredepa;
Vapreotide;
Verteporfin;
Vinblastine Sulfate;
Vincristine Sulfate;
Vindesine;
Vindesine Sulfate;
Vinepidine Sulfate;
Vinglycinate Sulfate;
Vinleurosine Sulfate;
Vinorelbine Tartrate;
Vinrosidine Sulfate;
Vinzolidine Sulfate;
Vorozole;
Zeniplatin;
Zinostatin;
Zorubicin Hydrochloride, 20-epi-1,25 dihydroxyvitamin D3;
5-ethynyluracil;
abiraterone, aclarubicin;
acylfulvene;
adecypenol;
adozelesin;
aldesleukin;
ALL-TK antagonists;
altretamine;
ambamustine;
amidox;
amifostine;
aminolevulinic acid;
amrubicin;
atrsacrine;
anagrelide;
anastrozole; and
rographolide;
angiogenesis inhibitors;
antagonist D;
antagonist G;
DHEA;
bromineepiandrosterone;
epiandrosterone;
antarelix;
anti-dorsalizing morphogenetic protein-1;
antiandrogen, prostatic carcinoma;
antiestrogen;
antineoplaston;
antisense oligonucleotides;
aphidicolin glycinate;
apoptosis gene modulators;
apoptosis regulators;
apurinic acid;
ara-CDP-DL-PTSA, arginine deaminase;
asulacrine;
atamestane;
atrimustine;
axinastatin 1;
axinastatin 2;
axinastatin 3;
azasetron;
azatoxin;
azatyrosine;
baccatin III derivatives;
balanol;
batimastat, BCR/ABL antagonists;
benzochlorins;
benzoylstaursporine;
beta lactam derivatives;
beta-alethine;
betaclamycin B;
betulinic acid;
bFGF inhibitor, bicalutamide;
bisantrene;
bisazindinylspermine;
bisnafide;
bistratene A;
bizelesin;
breflate;
bropirimine;
budotitane;
buthionine sulfoximine;
calcipotriol;
calphostin C;
camptothecin derivatives;
canarypox IL-2;
capecitabine;
carboxamide-amino-triazole;
carboxyamidotriazole;
CaRest M3;
CARN 700;
cartilage derived inhibitor;
carzelesin;
casein kinase inhibitors (ICOS);
castanospermine;
cecropin B;
cetrorelix;
chlorins;
chloroquinoxaline sulfonamide;
cicaprost;
cis-porphyrin;
cladribine;
clomifene analogues;
clotrimazole;
collismycin A;
collismycin B;
combretastatin A4;
combretastatin analogue;
conagenin;
crambescidin 816;
crisnatol;
cryptophycin 8;
cryptophycin A derivatives;
curacin A;
cyclopentanthrequinones;
cycloplatam;
cypemycin;
cytarabine ocfosfate;
cytolytic factor;
cytostatin;
dacliximab;
decitabine;
dehydrodidemnin B;
deslorelin;
dexifostamide;
dexrazoxane;
dexverapamil;
diaziquone;
didemnin B;
didox;
diethylnorspermine;
dihydro-5-azacytidine;
dihydrotaxol, 9-;
dioxamycin;
diphenyl spiromustine;
docosanol;
dolasetron;
doxifluridine;
droloxifene;
dronabinol;
duocannycin SA;
ebselen;
ecomustine;
edelfosine;
edrecolomab;
eflornithine;
elemene;
emitefur;
epirubicin;
epristeride;
estramustine analogue;
estrogen agonists;
estrogen antagonists;
etanidazole;
etoposide phosphate;
exemestane;
fadrozole;
fazarbine;
fenretinido;
filgrastim;
frnasteride;
flavopiridol;
flezelastine;
fluasterone;
fludarabine;
fluorodaunorunicin hydrochloride;
torfenimex;
formestane;
fostriecin;
fotemustine;
gadolinium texaphyrin;
gallium nitrate;
galocitabine;
ganirelix;
gelatinase inhibitors;
gemcitabine;
glutathione inhibitors;
hepsulfam;
heregulin;
hexamethylene bisacetamide;
hypericin;
ibandronic acid;
idarubicin;
idoxifene;
idramantone;
ilmofosine;
ilomastat;
imidazoacridones;
imiquimod;
immunostimulant peptides;
insulin-like growth factor-1 receptor inhibitor;
interferon agonists, interferons;
interleukins;
iobonguane;
iododoxorubicin;
ipomeanol, 4;
trinotecan;
iroplact;
irsogladine;
isobengazole;
isohomohalicondrin B;
itasetron;
jasplakinolide;
kahalalide F;
lamellarin-N triacetate;
lanreotide;
leinamycin;
lenograstim;
lentinan sulfate;
leptolstatin;
letrozole;
leukemia inhibiting factor;
leukocyte alpha interferon;
leuprolide+estrogen+progesterone;
leuprorelin;
levamisole liarozole;
linear polyamine analogue;
lipophilicadisaccharide peptide;
lipophilic platinum compounds;
lissoclinamide-7;
lobaplatin, lombricine;
lometrexol;
lonidamine;
losoxantrone;
lovastatin;
loxoribine;
lurtotecan;
lutetium texaphyrin;
lysofylline;
lytic peptides;
maitansine;
mannostatin A;
marimastat;
masoprocol;
maspin;
matrilysin inhibitors;
matrix metalloproteinase inhibitors;
menogaril;
merbarone;
meterelin;
methioninase;
metoclopramide;
MIF inhibitor;
mifepristone;
miltefosine;
mirimostim;
mismatched double stranded RNA;
mitoguazone;
mitolactol;
mitomycin analogues;
mitonafide;
mitotoxin fibroblast growth factor-saporin;
mitoxantrone;
mofarotene;
molgramostim;
monoclonal antibody, human chorionic gonadotrophin;
monophosplioryl lipid A+myobacterium cell wall sk;
mopidamol;
multiple drug resistance genie inhibitor;
multiple tumor suppressor 1-based therapy;
mustard anticancer agent;
mycaperoxide B;
mycobacterial cell wall extract;
myriaporone;
N-acetyldinaline;
N-substituted benzamides;
nafarelin;
nagrestip;
naloxone+pentazocine;
napavin;
naphterpin;
nartograstim;
nedaplatin;
nemorubicin;
neridronic acid;
neutral endopeptidase;
nilutamide;
nisamycin;
nitric oxide modulator;
nitroxide antioxidant;
nitrullyn;
O6-benzylguanine;
octreotide;
okicenone;
oligonucleotides;
onapristone;
orldarisetron;
ondansetron;
oracin;
oral cytokine inducer;
ormaplatin;
osaterone;
oxaliplatin;
oxaunomycin;
paclitaxel analogues;
paclitaxel derivatives;
palauamine;
palmitoylrhizoxin;
pamidronic acid;
panaxytriol;
panomifene;
parabactin;
pazelliptine;
pegaepergase;
peldesine;
pentosan polysulfate sodium;
pentostatin;
pentrozole;
perflubron;
perfosfamide;
perillyl alcohol;
phenazinomycin;
phenylacetate;
phosphatase inhibitors;
picibanil;
pilocarpine hydrochloride;
pirarubicin;
piritrexim;
placetin A;
placetin B;
plasminogen activator inhibitor;
platinum comprex;
platinum compounds;
platinum-triamine coil iplex;
porfimer sodium;
portiromycin;
propyl bis-acridone;
prostaglandin J2;
proteasome inhibitors;
protein A-based immune modulator;
protein kinase C inhibitor;
protein kinase C inhibitors, microalgal;
protein tyrosine phosphatase inhibitors;
purino mucleoside phosphorylast inhibitors;
purpurins;
pyrazoloacridine;
pyridoxylated hemoglobin polyoxyethylene conjugate;
raf antagonists;
raltitrexed;
ramosetron;
ras farnesyl protein transferase inhibitors;
ras inhibitor,;
ras-GAP inhibitor, retalliptine demethylated;
rhenium Re186 etidronate;
rhizoxin;
ribozymes;
RII retinamide;
rogletimide;
rohitukine;
romurtide;
roquinimex;
rubiginone B1;
ruboxyl;
safingol;
saintopin;
SarCNU;
sarcophytol A;
sargramostim, Sdi 1 mimetics;
semustine;
senescence derived inhibitor 1;
sense oligonucleotides;
signal transduction inhibitors;
signal transduction modulators;
single chain antigen binding protein;
sizofiran;
sobuzoxane;
sodium borocaptate;
sodium phenylacetate;
solverol;
somatomedin binding protein;
sonermin;
sparfosic acid;
spicamycin D;
spiromustine;
splenopentin;
spongistatin 1;
squalamine;
stem cell inhibitor;
stem-cell division inhibitors;
stipiamide;
stromelysin inhibitors;
sulfmonine;
superactive vasoactive intestinal peptide antagonist;
suradista;
suramin;
swainsonine;
synthetic glycosaminoglycans;
tallimustine;
tamoxifen methiodide;
tauromustine;
tazarotene;
tecogalan sodium;
tegafur;
tellurapyrylium;
telomerase inhibitors;
temoporfin;
temozolomide;
teniposide;
tetrachlorodecaoxide;
tetrazomine;
thaliblastine;
thalidomide;
thiocoraline;
thrombopoietin;
thrombopoietin mimetic;
thymalfasin;
thymopoietin receptor agonist;
thymotrinan;
thyroid stimulating hormone;
tin ethyl etiopurpurin;
tirapazamine;
titanocene dichloride;
topotecan;
topsentin;
toremifene;
totipotent stem cell factor;
translation inhibitors;
tretinoin;
triacetyluridine;
triciribine;
trimetrexate;
triptorelin;
tropisetron;
turosteride;
tyrosine kinase inhibitors;
tyrphostins;
UBC inhibitors;
ubenimex;
urogenital sinus-derived growth inhibitory factor;
urokinase receptor antagonists;
vapreotide;
variolin B;
vector system, erytrocyte gene therapy;
velaresol;
venom, anti-venom, veramine;
verdins;
verteporfin;
vinorelbine;
vinxaltine;
vitaxin;
vorozole;
zanoterone;
zeniplatin;
zilascorb;
zinostatin stimalamer, immunostimulating drugs or therapeutic agents, their metabolites, salts and derivatives thereof.
- antimetabolites and cytotoxic agents, such as daunorubicin, flourouracil, floxuridine, interferon alpha, methotrexate, plicamycin, mecaptopurine, thioguanine, adramycin, carmustine, lomustine, cytarabine, cyclophosphamide, doxorubicin, estramustine, altretamine, hydroxyurea, ifosfamide, procarbazine, mutamycin, busulfan, mitoxantrone, carboplatin, cisplatin, streptozocin, bleomycin, dactinomycin and idamycin, hormones such as, medroxyprogesterone, estramustine, ethinyl oestradiol, oestradiol, leuprolide, megestrol, octreotide, diethylstilbestrol, chlorotrianisene, etoposide, podophyllotoxin, and goserelin, nitrogen mustard derivatives such as, melphalan, chlorambucil, methlorethamine and thiotepa, steroids such as, betamethasone, and other antineoplastic agents such as live Mycobacterium bovis, dicarbazine, asparaginase, leucovoribn, mitotane, vincristine, vinblastine and texotere, cydophosphamide, adriamycin, 5-flourouracil, hexamethylmelamine, Acivicin;
-
53. The use of a pharmaceutical formulation as claimed in claims 50 to 52, wherein the pharmaceutical formulation is administered in combination with radiation treatment.
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54. The use of a pharmaceutical formulation as claimed in claims 50 to 53, wherein the pharmaceutical formulation is administered in combination with surgery.
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55. The use of a pharmaceutical formulation as claimed in claims 50 to 54, wherein the neoplasia is a precancerous lesion including syndromes represented by abnormal neoplastic and/or dysplastic, changes of tissue comprising precancerous growths in colonic, breast, renal, central nervous, gastric, or lung tissues, or conditions such as dysplastic nevus syndrome, a precursor to malignant melanoma of the skin, dysplastic nevus syndromes, polyposis syndromes, colonic polyps, precancerous lesions of the cervix (i.e., cervical dysplasia), prostatic dysplasia, bronchial dysplasia, breast, bladder and/or skin and related conditions (e.g., actinic keratosis), whether the lesions are clinically identifiable or not.
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56. The use of a pharmaceutical formulation as claimed in claims 50 to 55, wherein the neoplasia is prostate cancer, colon cancer, small cell lung cancer, large cell lung cancer, lung adenocarcinoma, epidermoid lung cancer, melanoma (including amelanotic subtypes), renal cell carcinoma, gastric carcinoma, cancers of the central nervous system including brain tumours, neuroblastomas, gastric carcinoma, breast cancer, ovarian cancer, testicular cancer, lymphoma and leukaemia, oesophageal cancer, stomach cancer, liver cancers, prostate cancer, cervical cancer, adrenal cancer, oral or mucosal cancer, bladder cancer, pancreatic cancer, lymphoma, Hodgkins disease, sarcomas, Hematopoeitic cell cancers such as B cell leukaemia/lymphomas, myelomas, T-cell leukemias/lymphomas, small cell leukemias/lymphomas, null cell, sezary, monocytic, myolomonocytic and Hairy cell leukemias.
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57. The use of a pharmaceutical formulation as claimed in claims 50 to 56, wherein the neoplasia is in the form of a tumour comprising an epidermoid and myeloid tumour, acute or chronic, nonsmall cell, squamous or solid.
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58. The use of a pharmaceutical formulation as claimed in claims 50 to 57, wherein the composition is micronized.
-
59. The use of a pharmaceutical formulation as claimed in claims 50 to 58, wherein the pharmaceutical formulation has an enteric coating.
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60. The use of a pharmaceutical formulation as claimed in claim 59, wherein the enteric coating is made of a polymer or copolymer.
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61. The use of a pharmaceutical formulation as claimed in claim 60, wherein the polymer or copolymer is selected from the group consisting of poly(lactic-glycolic acid) polyester, cellulose acetate phthalate, hydroxypropyl-methyl cellulose phthalate poly(butyl methacrylate), (2-dimethyl aminoethyl) methacrylate, and methyl methacrylate.
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62. The use of a pharmaceutical formulation as claimed in claims 50 to 61, wherein, the pharmaceutical formulation is administered enterally, parenterally, topically, orally, sublingually, rectally, nasally or vaginally.
-
63. The use of a pharmaceutical formulation as claimed in claims 50 to 62, wherein the composition is formulated into liposomes or carbohydrate vehicles.
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64. The use of a pharmaceutical formulation as claimed in claim 63, wherein the liposomes or carbohydrate vehicles are specifically targeted to tumours by covalently attaching a monoclonal antibody directed to a tumour-associated antigen.
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65. The use of a pharmaceutical formulation as claimed in claims 50 to 64, wherein the pharmaceutical formulation is administered intermittently.
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66. The use of a pharmaceutical formulation as claimed in claims 50 to 65, wherein the pharmaceutical formulation is a unit dose that comprises 5-500 mg of active ingredient consisting of at least one compound of the present invention.
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67. The use of a pharmaceutical formulation as claimed in claims 50 to 66, wherein the pharmaceutical formulation is administered to a mammal.
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68. The use of a pharmaceutical formulation as claimed in claim 67, wherein said mammal is a neonate and said administering is effected prior to delivery of said neonate and/or during delivery of said neonate.
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69. The use of a pharmaceutical formulation as claimed in claims 50 to 68, wherein the composition acts as a prodrug.
-
2. The composition as claimed in claim 1, wherein the compounds of the present invention are selected from the group comprising:
Specification
- Resources
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Current AssigneeElizabeth Shanahan-Prendergast
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Original AssigneeElizabeth Shanahan-Prendergast
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InventorsShanahan-Prendergast, Elizabeth
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Application NumberUS10/250,535Publication NumberTime in Patent OfficeDaysField of SearchUS Class Current514/469CPC Class CodesA61K 31/00 Medicinal preparations cont...A61K 31/015 carbocyclicA61K 31/343 condensed with a carbocycli...A61K 45/06 Mixtures of active ingredie...A61P 31/04 Antibacterial agentsA61P 31/12 AntiviralsA61P 33/00 Antiparasitic agentsA61P 35/00 Antineoplastic agentsA61P 37/00 Drugs for immunological or ...Y02A 50/30 Against vector-borne diseas...