METAL COORDINATED COMPOSITIONS

• US 20110275792A1
• Filed: 07/15/2011
• Published: 11/10/2011
• Est. Priority Date: 10/25/2004
• Status: Active Grant

• Current Assignee: Synthonics Incorporated (Synthonics Technologies, Inc.)
• Original Assignee: Synthonics Incorporated (Synthonics Technologies, Inc.)
• Inventors: Piccariello, Thomas
• Granted Patent: US 8,389,726 B2
• Time in Patent Office: Days
• US Class Current: 530/397
• CPC Class Codes: A61K 47/52 the modifying agent being an inorganic compound, e.g. an inorganic ion that is complexed with the active ingredient
• CPC Class Codes: A61K 47/547 Chelates, e.g. Gd-DOTA or Zinc-amino acid chelates; Chelate-forming compounds, e.g. DOTA or ethylenediamine being covalently linked or complexed to the pharmacologically- or therapeutically-active agent
• CPC Class Codes: A61K 47/55 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• CPC Class Codes: A61K 47/552 one of the codrug's components being an antibiotic
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 13/04 for urolithiasis
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/10 for petit-mal
• CPC Class Codes: A61P 25/12 for grand-mal
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 27/02 : Ophthalmic agents
• CPC Class Codes: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 : for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/04 : Antibacterial agents
• CPC Class Codes: A61P 31/12 : Antivirals
• CPC Class Codes: A61P 35/00 : Antineoplastic agents
• CPC Class Codes: A61P 37/06 : Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/14 : of the thyroid hormones, e.g. T3, T4
• CPC Class Codes: A61P 7/02 : Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 7/06 : Antianaemics
• CPC Class Codes: A61P 7/10 : Antioedematous agents; Diuretics
• CPC Class Codes: A61P 9/12 : Antihypertensives
• CPC Class Codes: C07F 3/003 : without C-Metal linkages
• CPC Class Codes: C07F 3/02 : Magnesium compounds
• CPC Class Codes: C07F 3/06 : Zinc compounds
• CPC Class Codes: C07H 21/02 : with ribosyl as saccharide radical

Abstract

A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.

Claims

1-47. -47. (canceled)

48. A metal coordination complex of a biologically active moiety and a metal, wherein:

the biologically active moiety is selected from the group consisting of Zanamivir, Levofloxacin, Montelukast, Epoetin, Enalapril, Methotrexate, Hydralazine, Metronidazole, Carbergoline, Gentamycin, Tobramycin, Acarbose, interference ribonucleic acid (iRNA), Atorvastatin, Lansoprazole, Losartan, Olanzapine, Gabapentin, Pemetrexed, Tenofovir, Ramipril, Trovafloxacin, and derivatives thereof; and

wherein the metal is selected from the group consisting of aluminum, bismuth, calcium, copper, iron, magnesium, silicon, and zinc.

49. The invention of claim 48 wherein the biologically active moiety is selected from the group consisting of Zanamivir, Levofloxacin, Montelukast, Epoetin, Enalapril, Methotrexate, Hydralazine, Metronidazole, Carbergoline, Gentamycin, Tobramycin, Acarbose, and derivatives thereof.

50. The invention of claim 48 wherein the biologically active moiety is selected from the group consisting of iRNA, Atorvastatin, Lansoprazole, Losartan, Olanzapine, Gabapentin, Pemetrexed, and derivatives thereof.

51. The invention of claim 48 wherein the biologically active moiety is selected from the group consisting of Tenofovir, Ramipril, Trovafloxacin, and derivatives thereof.

52. The invention of claim 48 wherein the biologically active moiety is selected from the group consisting of antidiabetics, antiGERDs, antineoplastics, antivirals, antihypertensives, antibiotics, antiparkinsonians, hormone replacements, diuretics, antipsoriatics, antirheumatics, antiepileptics, antidepressants, and analgesics.

53. The invention of claim 48 wherein the biologically active moiety comprises a guanide functionality, a diamine functionality or a combination thereof.

54. The invention of claim 48 wherein the biologically active moiety comprises Zanamavir.

55. The invention of claim 54 wherein the metal is selected from the group consisting of calcium, copper, magnesium, and zinc.

56. The invention of claim 54 wherein the metal comprises copper.

57. A method of modulating properties of a biologically active moiety comprising:

forming a metal coordination complex of the biologically active moiety with a metal;

wherein the biologically active moiety is selected from the group consisting of Zanamivir, Levofloxacin, Montelukast, Epoetin, Enalapril, Methotrexate, Hydralazine, Metronidazole, Carbergoline, Gentamycin, Tobramycin, Acarbose, iRNA, Atorvastatin, Lansoprazole, Losartan, Olanzapine, Gabapentin, Pemetrexed, Tenofovir, Ramipril, Trovafloxacin, and derivatives thereof; and

wherein the metal is selected from the group consisting of aluminum, bismuth, calcium, copper, iron, magnesium, silicon, and zinc.

58. The invention of claim 57 wherein the biologically active moiety is selected from the group consisting of Zanamivir, Levofloxacin, Montelukast, Epoetin, Enalapril, Methotrexate, Hydralazine, Metronidazole, Carbergoline, Gentamycin, Tobramycin, Acarbose, and derivatives thereof.

59. The invention of claim 57 wherein the biologically active moiety is selected from the group consisting of iRNA, Atorvastatin, Lansoprazole, Losartan, Olanzapine, Gabapentin, Pemetrexed, and derivatives thereof.

60. The invention of claim 57 wherein the biologically active moiety is selected from the group consisting of Tenofovir, Ramipril, Trovafloxacin, and derivatives thereof.

61. The invention of claim 57 wherein the biologically active moiety is selected from the group consisting of antidiabetics, antiGERDs, antineoplastics, antivirals, antihypertensives, antibiotics, antiparkinsonians, hormone replacements, diuretics, antipsoriatics, antirheumatics, antiepileptics, antidepressants, and analgesics.

62. The invention of claim 57 wherein the biologically active moiety comprises a guanide functionality, a diamine functionality or a combination thereof.

63. The invention of claim 57 wherein the biologically active moiety comprises Zanamavir.

64. The invention of claim 63 wherein the metal is selected from the group consisting of bismuth, copper, magnesium, and zinc.

65. The invention of claim 63 wherein the metal comprises copper.

66. The method of claim 57 wherein the properties to be modulated are selected from the group consisting of potency, stability, absorbability, targeted delivery, and combinations thereof.

67. A metal coordination complex of a biologically active moiety and a metal, wherein:

the biologically active moiety is selected from the group consisting of Zanamivir, Levofloxacin, Montelukast, Epoetin, Enalapril, Methotrexate, Hydralazine, Metronidazole, Carbergoline, Gentamycin, Tobramycin, Acarbose, and derivatives thereof; and

wherein the metal is selected from the group consisting of aluminum, bismuth, calcium, copper, iron, magnesium, silicon, and zinc.

68. The invention of claim 67 wherein the biologically active moiety is selected from the group consisting of Zanamavir, Levofloxacin, and Montelukast.

69. The invention of claim 68 wherein the biologically active moiety comprises Zanamavir.