LIPID-BASED PLATINUM COMPOUNDS AND NANOPARTICLES

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum based compounds, nanoparticles and compositions comprising said platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid carbene compounds, platinum based compounds, nanoparticles and compositions thereof. 1. A compound comprising:(a) a platinum moiety; and(b) a lipid connected to said platinum moiety.2. The compound of claim 1 , wherein the compound comprises a carbonyl moiety.3. The compound of claim 2 , wherein the carbonyl moiety is a carboxylic acid that is succinic acid claim 2 , malonic acid claim 2 , oxalic acid claim 2 , keto acid claim 2 , or a combination thereof4. The compound of claim 1 , wherein the platinum moiety comprises a platinum atom that is conjugated to said lipid via covalent bond claim 1 , coordinate bond or a combination thereof.5. The compound of claim 1 , further comprising at least one linker between the platinum moiety and the lipid.7. The compound of claim 1 , wherein the linker is:{'sub': 2', '2', '1, 'claim-text': X is NH;', {'sub': 1', '2, 'Xis C(O)O, C(O)NH, O(CH)—O, NH, or O;'}, {'sub': 2', '2', 'n, 'Xis (CH)or C(O); and'}, 'n is 0, 1, 2, 3, 4, or 5;, '(i) —X—CH—X—X—, wherein{'sub': 2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'm', '2', 'n', '2', 'm', '2', 'n', '2', 'n', '2', 'm', '2', 'n, 'claim-text': 'wherein, n and m are, independently, 0, 1, 2, 3, 4, or 5;', '(ii) —(CH)O—, —(CH)NHC(O)O—, —(CH)OC(O)NH—, —(CH)C(O)NH(CH)O—, —(CH)O(CH)O—, —(CH)OC(O)—, (CH)NHC(O)(CH)O—, or —(CH)C(O)O—;'}{'sub': 3', '4', '5', '6, 'claim-text': [{'sub': 3', '2, 'Xis CH, CH, or O; and'}, {'sub': 4', '5', '6', '2, 'X, Xand Xare, independently, —CHO— or O; or'}], '( ...

PROCESS FOR PREPARING SUPRAMOLECULAR PLATINUM-BASED COMPOUNDS

The present invention is in relation to the fields of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to improved methods for preparing lipid-conjugated platinum compounds with high purity and good yields. The present disclosure also relates to nanoparticles comprising lipid-conjugated platinum compounds with high drug loading efficiency for use in chemotherapy, and to methods for producing said nanoparticles. 1. A method for preparing a lipid-conjugated platinum compound comprising:reacting a water-soluble salt of a lipid with a water-soluble platinum compound in a substantially aqueous solution to obtain the lipid-conjugated platinum compound as a precipitate;wherein the method provides a yield of >50% for the lipid-conjugated platinum compound; andwherein the method provides a purity of >70% for the lipid-conjugated platinum compound.2. The method of claim 1 , further comprising the step of:filtering or centrifuging the reaction mixture to separate the precipitate from the substantially aqueous solution, and optionally washing the precipitate with water.3. The method of or claim 1 , further comprising the step of:purifying the lipid-conjugated platinum compound using HPLC.4. The method of any one of - claim 1 , wherein the purity of the lipid-conjugated platinum compound is determined using analytical HPLC on a NH claim 1 , C18 or Phenyl column.5. The method of claim 3 , wherein the HPLC purification uses a preparative reverse-phase column.6. The method of claim 5 , wherein the column comprises an NHstationary phase claim 5 , a Phenyl stationary phase claim 5 , or a C18 stationary phase.7. The method of any one of - claim 5 , wherein the column comprises NHor Phenyl stationary phase claim 5 , and the lipid-conjugated platinum compound is eluted using a gradient method.8. The method of claim 7 , wherein the gradient method comprises eluting with a mobile phase comprising a mixture of water and methanol claim 7 , wherein ...

LIPID-BASED PLATINUM-N-HETEROCYCLIC CARBENE COMPOUNDS AND NANOPARTICLES

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to carbene compounds, particularly platinum containing carbenes and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum containing carbenes, nanoparticles and compositions comprising said platinum containing carbenes/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid platinum based compounds, nanoparticles and compositions. 2. (canceled)3. (canceled)4. The compound of claim 1 , wherein the carbene is abnormal or normal N-heterocyclic-carbene platinum(II) compound.5. The compound of claim 1 , wherein the compound comprises a lipid.6. The compound of claim 5 , wherein the platinum atom is conjugated to said lipid via covalent bond claim 5 , coordinate bond or a combination thereof.7. The compound of claim 5 , wherein the compound comprises at least one linker between the platinum moiety and the lipid.8. The compound of claim 7 , wherein the linker is selected from the group consisting of:{'sub': 2', '2', '1', '1', '2', '2', '2', 'n, '(i) —X—CH—X—X—, wherein X is NH; Xis C(O)O, C(O)NH, O(CH)—O, NH, or O; Xis (CH)or C(O); and n is 0, 1, 2, 3, 4, or 5;'}{'sub': 2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'm', '2', 'n', '2', 'm', '2', 'n', '2', 'n', '2', 'm', '2', 'n, '(ii) —(CH)O—, —(CH)NHC(O)O—, —(CH)OC(O)NH—, —(CH)C(O)NH(CH)O—, —(CH)O(CH)O—, —(CH)O(O)—, —(CH)NHC(O)(CH)O—, or —(CH)C(O)O—; wherein n and m are independently 0, 1, 2, 3, 4, or 5;'}{'sub': 3', '4', '5', '6', '3', '2', '4', '5', '6', '2, '(iii) —X—XX—X, wherein Xis CH, CH, or O; and X, Xand Xare independently same or different and are —CHO— or O; and'}(iv) any combinations of (i)-(iii).9. The compound of claim 7 , wherein the linker is selected from the group consisting of: a bond claim 7 , ethylene diamine claim 7 , ethylene glycol claim 7 , diethylene glycol claim 7 , 1 claim 7 ,3 ...

LIPID-BASED PLATINUM COMPOUNDS AND NANOPARTICLES

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum based compounds, nanoparticles and compositions comprising said platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid carbene compounds, platinum based compounds, nanoparticles and compositions thereof. 1. A compound comprising:(a) a platinum moiety; and(b) a lipid connected to said platinum moiety.2. The compound of claim 1 , wherein the compound comprises a carbonyl moiety.3. The compound of claim 2 , wherein the carbonyl moiety is a carboxylic acid selected from the group consisting of succinic acid claim 2 , malonic acid claim 2 , oxalic acid claim 2 , keto acid claim 2 , and any combination thereof.4. The compound of claim 1 , wherein the platinum atom is conjugated to said lipid via covalent bond claim 1 , coordinate bond or a combination thereof.5. The compound of claim 1 , wherein the compound comprises at least one linker between the platinum moiety and the lipid.9. (canceled)10. The compound of claim 5 , wherein the linker is selected from the group consisting of:{'sub': 2', '2', '1', '1', '2', '2', '2', 'n, '(i) —X—CH—X—X—, wherein X is NH; Xis C(O)O, C(O)NH, O(CH)—O, NH, or O; Xis (CH)or C(O); and n is 0, 1, 2, 3, 4, or 5;'}{'sub': 2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'm', '2', 'n', '2', 'm', '2', 'n', '2', 'n', '2', 'm', '2', 'n, '(ii) —(CH)O—, —(CH)NHC(O)O—, —(CH)OC(O)NH—, —(CH)C(O)NH(CH)O—, —(CH)O(CH)O—, —(CH)O(O)—, —(CH)NHC(O)(CH)O—, or —(CH)C(O)O—; wherein n and m are independently 0, 1, 2, 3, 4, or 5;'}{'sub': 3', '4', '5', '6', '3', '2', '4', '5', '6', '2, '(iii) —X—XX—X, wherein Xis CH, CH, or O; and X, Xand Xare independently same or different and ...

FLUORESCENT ANTICANCER PLATINUM DRUGS

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to fluorescent platinum based compounds. The disclosure further relates to synthesis of said fluorescent platinum based compounds, nanoparticles and compositions comprising said fluorescent platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by the fluorescence changes between aforesaid platinum based compounds and corresponding free ligands, nanoparticles and compositions. 153-. (canceled)54. A platinum containing complex comprising:(a) a fluorescent molecule; and(b) platinum atom conjugated with the fluorescent molecule.57. The complex of claim 54 , wherein the platinum atom is conjugated to the fluorescent molecule via a covalent bond claim 54 , coordinate bond or a combination thereof.62. The complex of claim 54 , wherein the compound exhibits increased cellular uptake of platinum relative to cisplatin or oxaliplatin in cancer cells; or the complex exhibits a higher accumulation of platinum in a tumor relative to cisplatin or oxaliplatin at an equivalent dosage amount of amount of cisplatin or oxaliplatin.65. The compound of claim 63 , wherein the wherein the lipid is selected from fats claim 63 , waxes claim 63 , sterols claim 63 , steroids claim 63 , bile acids claim 63 , fat-soluble vitamins claim 63 , monoglycerides claim 63 , diglycerides claim 63 , phospholipids claim 63 , glycolipids claim 63 , sulpholipids claim 63 , aminolipids claim 63 , chromolipids claim 63 , glycerophospholipids claim 63 , sphingolipids claim 63 , prenol lipids claim 63 , saccharolipids claim 63 , polyketides and fatty acids or any combination thereof claim 63 , preferably the lipid is cholesterol; lumisterol claim 63 , alpha-tocopherol or vitamin A; wherein the sterol is selected from cholesterol claim 63 , cholesterol chloroformate or derivatives thereof claim 63 , and any combination thereof; ...

CRYSTALLINE PLATINUM-BASED COMPOUNDS

The present disclosure relates to pharmaceutical sciences and chemical sciences. In particular, the present disclosure provides crystalline platinum-based compound IO-125, compositions and formulations comprising the same, along with method of preparing said crystalline compound, and uses thereof. 2. The crystalline form 1 of claim 1 , having a melting point of about 320° C. and purity of about 97%.3. The crystalline form 1 of claim 1 , that is characterized by a powder X-ray diffraction spectrum substantially as shown in claim 1 , claim 1 , claim 1 , claim 1 , or claim 1 , a coupled thermogravimetric/differential thermal analysis thermogram substantially as shown in claim 1 , or a high performance liquid chromatography chromatogram substantially as shown in .4. A method for preparing the crystalline Form 1 of claim 1 , comprising:(i) dissolving crude IO-125 in at least one solvent to form a solution;(ii) crystallizing the crystalline Form 1 from the solution; and(iii) optionally repeating step (ii).5. The method of claim 4 , wherein the solvent is a lower alkyl alcohol claim 4 , halogenated hydrocarbon claim 4 , inorganic solvent claim 4 , an organic solvent claim 4 , or a combination thereof.6. The method of claim 5 , wherein the lower alkyl alcohol is methanol claim 5 , ethanol claim 5 , propanol claim 5 , isopropanol claim 5 , butanol claim 5 , iso-butanol claim 5 , pentanol claim 5 , iso-pentanol claim 5 , or a combination thereof; the halogenated hydrocarbon solvent is dichloromethane claim 5 , chloroform claim 5 , or a combination thereof; the inorganic solvent is water; and the organic solvent is dimethylformamide.7. The method of claim 4 , wherein the solvent is a methanol and dichloromethane mixture claim 4 , methanol and chloroform mixture claim 4 , ethanol and dichloromethane mixture claim 4 , ethanol and chloroform mixture claim 4 , or a combination thereof.8. The method of claim 4 , wherein the solvent is chloroform claim 4 , a methanol and ...

LIPID-BASED PLATINUM COMPOUNDS AND NANOPARTICLES

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum based compounds, nanoparticles and compositions comprising said platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid carbene compounds, platinum based compounds, nanoparticles and compositions thereof. 1. A compound comprising:(a) a platinum moiety; and(b) a lipid connected to said platinum moiety.2. The compound of claim 1 , (i) wherein the compound comprises a carbonyl moiety; or (ii) wherein the platinum moiety comprises a platinum atom that is conjugated to said lipid via covalent bond claim 1 , coordinate bond or a combination thereof; or (iii) further comprising at least one linker between the platinum moiety and the lipid.3. The compound of claim 1 , wherein the carbonyl moiety is a carboxylic acid that is succinic acid claim 1 , malonic acid claim 1 , oxalic acid claim 1 , keto acid claim 1 , or a combination thereof5. The compound of claim 1 , wherein the linker is:{'sub': 2', '2', '1, 'claim-text': X is NH;', {'sub': 1', '2, 'Xis C(O)O, C(O)NH, O(CH)—O, NH, or O;'}, {'sub': 2', '2', 'n, 'Xis (CH)or C(O); and'}, 'n is 0, 1, 2, 3, 4, or 5;, '(i) —X—CH—X—X—, wherein{'sub': 2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'm', '2', 'n', '2', 'm', '2', 'n', '2', 'n', '2', 'm', '2', 'n, '(ii) —(CH)O—, —(CH)NHC(O)O—, —(CH)OC(O)NH—, —(CH)C(O)NH(CH)O—, —(CH)O(CH)O—, —(CH)OC(O)—, (CH)NHC(O)(CH)O—, or —(CH)C(O)O—; wherein, n and m are, independently, 0, 1, 2, 3, 4, or 5;'}{'sub': 3', '4', '5', '6, 'claim-text': [{'sub': 3', '2, 'Xis CH, CH, or O; and'}, {'sub': 4', '5', '6', '2, 'X, Xand Xare, independently, —CHO— or O; or'}], '(iii) —X—XX—X, wherein(iv) a combination of (i)-(iii).6 ...

COMPOUNDS AS LXR AGONISTS

The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.

Lipid-based platinum compounds and nanoparticles, their preparation processes, pharmaceutical compositions comprising the same and their uses in the treatment of cancer

COMPOSTOS E NANOPARTÍCULAS DE PLATINA COM BASE EM LIPÍDIO. A presente descrição se refere ao campo de nanotecnologia e agentes terapêuticos para o câncer. Em particular, a presente invenção se refere a compostos com base em platina que compreendem uma porção de platina, uma porção ligante e uma porção de lipídio e nanopartículas correspondentes dos mesmos. A descrição se refere ainda à síntese dos ditos compostos e nanopartículas com base em platina, e composições que compreendem os ditos compostos/nanopartículas com base em platina. A descrição também se refere a métodos de manejo de câncer ao empregar os compostos de carbeno, compostos com base em platina, nanopartículas e composições dos mesmos supracitados. PLATINUM COMPOUNDS AND NANOPARTICLES BASED ON LIPIDIUM. The present description pertains to the field of nanotechnology and therapeutic agents for cancer. In particular, the present invention relates to platinum-based compounds comprising a platinum moiety, a binding moiety and a lipid moiety and corresponding nanoparticles thereof. The description further relates to the synthesis of said platinum-based compounds and nanoparticles, and compositions comprising said platinum-based compounds/nanoparticles. The description also pertains to cancer management methods employing the aforementioned carbene compounds, platinum-based compounds, nanoparticles and compositions thereof.

process for the preparation of supramolecular platinum compounds

Crystalline platinum-based compounds

The present disclosure relates to pharmaceutical sciences and chemical sciences. In particular, the present disclosure provides crystalline platinum-based compound IO-125, compositions and formulations comprising the same, along with method of preparing said crystalline compound, and uses thereof.

Lipid-based platinum compounds and nanoparticles

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum based compounds, nanoparticles and compositions comprising said platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid carbene compounds, platinum based compounds, nanoparticles and compositions thereof.

Process for preparing lipid-conjugated platinum-based compounds

The present invention is in relation to the fields of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to improved methods for preparing lipid- conjugated platinum compounds with high purity and good yields. The present disclosure also relates to nanoparticles comprising lipid-conjugated platinum compounds with high drug loading efficiency for use in chemotherapy, and to methods for producing said nanoparticles.

Lipid-based platinum compounds and nanoparticles

The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum based compounds, nanoparticles and compositions comprising said platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid carbene compounds, platinum based compounds, nanoparticles and compositions thereof.