Provided herein are crystalline forms (forms I, II, IIA, IIB, IIC and IID) of a compound of formula (I) as defined herein. Also provided herein are processes for the production of crystalline forms I, II, IIA, IIB, IIC and IID, and pharmaceutical compositions and therapeutic methods involving crystalline form I.
C07D 303/40 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by ester radicals
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A01N 43/20 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom three- or four-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
A61K 9/00 - Medicinal preparations characterised by special physical form
C07D 303/14 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
C07D 303/17 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals containing oxirane rings condensed with carbocyclic ring systems having three or more relevant rings
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
C07D 303/44 - Esterified with oxirane-containing hydroxy compounds
Provided herein are combination therapies comprising an epoxytigliane compound (for example, tigilanol tiglate) and either irradiation or a chemotherapeutic agent that is i) a chemotherapeutic agent that damages DNA (for example, cisplatin), or ii) a chemotherapeutic agent that inhibits tumour-associated host-derived cells that support the growth and/or invasion of tumour cells (for example, 5-fluoruracil, or doxorubicin). Pharmaceutical compositions and kits containing epoxytigliane compounds and the chemotherapeutic agents are also provided.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
Provided herein is a crystalline intermediate useful in the manufacture of 6,7-epoxytigliane compounds. Methods of making the 6,7-epoxytigliane compounds using the crystalline intermediates are also provided, as well as high purity 6,7-epoxytigliane compounds that are able to be produced using the crystalline intermediate.
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
Provided herein is a crystalline intermediate useful in the manufacture of 6,7-epoxytigliane compounds. Methods of making the 6,7-epoxytigliane compounds using the crystalline intermediates are also provided, as well as high purity 6,7-epoxytigliane compounds that are able to be produced using the crystalline intermediate.
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
The present invention relates to methods of dispersing biofilms comprising Gram-negative bacteria, the methods comprising exposing the biofilm to an epoxytiglienone compound or a salt thereof. Methods of treating infections comprising the localised administration, for example, topically or by injection, of an epoxytiglienone compound into or onto an established biofilm comprising Gram-negative bacteria to disrupt the structure of that biofilm and methods of preventing biofilms comprising Gram-negative bacteria forming or dispersing biofilms comprising Gram-negative biofilms that have formed on medical devices are also described.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
The present invention relates to methods of treating tumours comprising the localised administration, for example, intratumourally or topically, of an epoxytiglienone compound (as a monotherapy) to cancerous tumours to generate a systemic anticancer abscopal (anenestic) and/or bystander effect.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention relates to methods of dispersing biofilms comprising Gram-negative bacteria, the methods comprising exposing the biofilm to an epoxytiglienone compound or a salt thereof. Methods of treating infections comprising the localised administration, for example, topically or by injection, of an epoxytiglienone compound into or onto an established biofilm comprising Gram-negative bacteria to disrupt the structure of that biofilm and methods of preventing biofilms comprising Gram-negative bacteria forming or dispersing biofilms comprising Gram-negative biofilms that have formed on medical devices are also described.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
The present invention relates to methods of dispersing biofilms comprising Gram-negative bacteria, the methods comprising exposing the biofilm to an epoxytiglienone compound or a salt thereof. Methods of treating infections comprising the localised administration, for example, topically or by injection, of an epoxytiglienone compound into or onto an established biofilm comprising Gram-negative bacteria to disrupt the structure of that biofilm and methods of preventing biofilms comprising Gram-negative bacteria forming or dispersing biofilms comprising Gram-negative biofilms that have formed on medical devices are also described.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
The present invention relates to methods of treating tumours comprising the localised administration, for example, intratumourally or topically, of an epoxytiglienone compound (as a monotherapy) to cancerous tumours to generate a systemic anticancer abscopal (anenestic) and/or bystander effect.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A61K 35/00 - Medicinal preparations containing materials or reaction products thereof with undetermined constitution
The present invention relates to methods of treating tumours comprising the localised administration, for example, intratumourally or topically, of an epoxytiglienone compound (as a monotherapy) to cancerous tumours to generate a systemic anticancer abscopal (anenestic) and/or bystander effect.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A61K 35/00 - Medicinal preparations containing materials or reaction products thereof with undetermined constitution
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A01N 43/20 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom three- or four-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
C07D 303/14 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
C07D 303/44 - Esterified with oxirane-containing hydroxy compounds
C07D 303/17 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals containing oxirane rings condensed with carbocyclic ring systems having three or more relevant rings
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention relates to a combination therapy for tumours comprising the administration of an epoxytigliane compound and an immune checkpoint inhibitor. In particular embodiments, there is a method of treating a tumour and/or treating or preventing one or more bystander tumours with the therapy. Pharmaceutical compositions and kits containing epoxytigliane compounds and immune checkpoint inhibitors are also described.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.
C07D 303/40 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by ester radicals
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A61K 8/49 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A01N 43/20 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom three- or four-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
C07D 303/14 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
C07D 303/44 - Esterified with oxirane-containing hydroxy compounds
C07D 303/17 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals containing oxirane rings condensed with carbocyclic ring systems having three or more relevant rings
A61K 9/00 - Medicinal preparations characterised by special physical form
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of solid tumors and chronic wounds in animals and humans; pharmaceutical preparations for veterinary use for the treatment of solid tumors and chronic wounds in animals; anticancer veterinary preparations
17.
COMBINATION THERAPY FOR THE TREATMENT OR PREVENTION OF TUMOURS
The present invention relates to a combination therapy for tumours comprising the administration of an epoxytigliane compound and an immune checkpoint inhibitor. In particular embodiments, there is a method of treating a tumour and/or treating or preventing one or more bystander tumours with the therapy. Pharmaceutical compositions and kits containing epoxytigliane compounds and immune checkpoint inhibitors are also described.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations, namely, preparations for treatment of tumors; pharmaceutical preparations for veterinary use, namely, preparations for treatment of tumors; veterinary preparations, namely, preparations for treatment of tumors
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for veterinary use for the treatment of cancer; veterinary preparations for the treatment of cancer
The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
C07D 303/40 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by ester radicals
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A61K 36/47 - Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
A61K 8/49 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A01N 43/20 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom three- or four-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
C07D 303/14 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
C07D 303/44 - Esterified with oxirane-containing hydroxy compounds
C07D 303/17 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals containing oxirane rings condensed with carbocyclic ring systems having three or more relevant rings
The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
C07D 303/40 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by ester radicals
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 36/47 - Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
A61K 8/49 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
A01N 43/20 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom three- or four-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
C07D 303/14 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A01N 43/20 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom three- or four-membered rings
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
C07D 303/00 - Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
